U.S. patent application number 13/181746 was filed with the patent office on 2011-12-29 for method of controlling pests with biosurfactant penetrants as carriers for active agents.
Invention is credited to Mohamed M. Awada, Salam M. Awada, Rex S. Spendlove.
Application Number | 20110319341 13/181746 |
Document ID | / |
Family ID | 35425557 |
Filed Date | 2011-12-29 |
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United States Patent
Application |
20110319341 |
Kind Code |
A1 |
Awada; Salam M. ; et
al. |
December 29, 2011 |
METHOD OF CONTROLLING PESTS WITH BIOSURFACTANT PENETRANTS AS
CARRIERS FOR ACTIVE AGENTS
Abstract
A penetrating composition can include an active agent that has
an activity that is either beneficial for plants or controls pests.
The composition can also include a penetrant that is present in an
effective amount for carrying the at least one active agent into or
through a medium, the medium being at least one of a plant, soil,
or pest. Also, penetrating composition can be used for increasing
the permeation of an active agent in an animal. The composition
includes an active agent having an activity that is beneficial for
an animal. Also, the composition includes a penetrant selected from
the group consisting of biosurfactants, glycolipids, lipopeptides,
favolipids, lipoproteins, phospholipids, lipopolysaccharide-protein
complexes, polysaccharide-protein-fatty acid complexes, and
combinations thereof. A biosurfactant composition can include an
effective amount of a biosurfactant for controlling a pest,
preserving a plant cutting, or reducing effects of environmental
stress on a plant.
Inventors: |
Awada; Salam M.; (Logan,
UT) ; Awada; Mohamed M.; (Logan, UT) ;
Spendlove; Rex S.; (Millville, UT) |
Family ID: |
35425557 |
Appl. No.: |
13/181746 |
Filed: |
July 13, 2011 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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11209132 |
Aug 22, 2005 |
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13181746 |
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11141669 |
May 31, 2005 |
7994138 |
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11209132 |
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60575913 |
Jun 1, 2004 |
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60604139 |
Aug 23, 2004 |
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Current U.S.
Class: |
514/20.9 ;
514/1.1; 514/148; 514/23; 514/772; 514/772.3; 514/772.4; 514/772.5;
514/773; 514/777; 514/784; 514/785 |
Current CPC
Class: |
A01N 25/30 20130101;
C05G 3/70 20200201; A01N 63/10 20200101; A01N 43/16 20130101 |
Class at
Publication: |
514/20.9 ;
514/773; 514/777; 514/785; 514/772; 514/772.5; 514/772.3;
514/772.4; 514/784; 514/1.1; 514/23; 514/148 |
International
Class: |
A01N 25/30 20060101
A01N025/30; A01N 43/04 20060101 A01N043/04; A01N 57/10 20060101
A01N057/10; A01P 7/02 20060101 A01P007/02; A01P 3/00 20060101
A01P003/00; A01P 7/04 20060101 A01P007/04; A01P 9/00 20060101
A01P009/00; A01P 1/00 20060101 A01P001/00; A01N 37/18 20060101
A01N037/18; A01N 43/16 20060101 A01N043/16 |
Claims
1. A method for controlling pests, the method comprising: obtaining
a homogeneous penetrating composition comprising: at least one
active agent in an effective amount to have an activity of
controlling a pest so as to kill, disable, and/or immobilize the
pest; and at least one biosurfactant penetrant selected from the
group of glycolipids, rhamnolipids, lipopeptides, flavolipids,
lipoproteins, phospholipids, lipopolysaccharide-protein complexes,
or polysaccharide-protein-fatty acid complexes having the at least
one active agent in the effective amount homogeneously dispersed
therein, the at least one biosurfactant penetrant being present in
an effective amount for carrying the at least one active agent in
the effective amount into or through the pest in order to control
the pest; and providing the homogeneous penetrating composition to
a pest in an amount such that the pest is substantially controlled
with the active agent.
2. The method as in claim 1, further comprising at least one
additional penetrant selected from the group consisting of
aliphatic sulfones, acyclic sulfones, sulfones, sulfoxides,
polyvinylpyrrolidone, and combinations thereof.
3. The method as in claim 1, wherein the at least one active agent
is selected from the group consisting of pesticides, elicitors,
biopesticides, biopesticide byproducts, and combinations
thereof.
4. The method as in claim 3, further comprising at least one
solubility controlling agent.
5. The method as in claim 4, wherein the solubility controlling
agent is selected from the group consisting of slow release
cross-linked swellable gel, slow release cross-linked swellable
polyacrylamide gel, wax, chitin, chitosan, C12-C20 fatty acid,
myristic acid, stearic acid, palmitic acid, C12-C20 alcohol, lauryl
alcohol, cetyl alcohol, myristyl alcohol, stearyl alcohol,
amphiphilic esters of fatty acids, glycerol, monoester C12-C20
fatty acids, glyceryl monolaurate, glyceryl monopalmitate, glycerol
esters of fatty acids, polyethylene monostearate,
polypropylenemonopalmitate glycols, C12-C20 amines, lauryl amine,
mystyl amine, stearyl amine, amide C12-C20 fatty acids, and
combinations thereof.
6. The method as in claim 3, wherein the at least one active agent
is complexed or chelated with the at least one biosurfactant
penetrant.
7. The method as in claim 1, wherein the biosurfactant penetrant is
selected from the group consisting of glycolipids, lipopeptides,
flavolipids, rhamnolipids, lipoproteins, phospholipids,
lipopolysaccharide-protein complexes, polysaccharide-protein-fatty
acid complexes and combinations thereof.
8. The method as in claim 1, wherein the biosurfactant penetrant is
a glycolipid and the active agent is a pesticide.
9. The method as in claim 1, wherein the composition is a liquid
homogenous composition.
10. The method as in claim 1, wherein the composition is a
homogeneous solid, or paste composition.
11. The method as in claim 1, comprising preparing the homogeneous
penetrating composition, the preparing comprising one or more of
the following: mixing for about 10 minutes; mixing under heat;
compression molding the homogeneous composition; tabletting the
homogeneous composition; pressing the homogeneous composition;
extruding the homogeneous composition; injection molding the
homogeneous composition; or liquefying the homogeneous
composition.
12. The method as in claim 1, wherein the biosurfactant is obtained
from a microbe selected from the group of: Pseudomonas species;
Flavobacterium species; Candida species; Rhodococcus species; or
Arthrobacter species.
13. The method of claim 1, further comprising cultivating a microbe
so as to produce the biosurfactant.
14. The method of claim 1, wherein the biosurfactant includes a
rhamnolipid and/or a sophorlipid.
15. The method of claim 1, wherein the pests are selected from
fungi, nematodes, leafminers, citrus leafminers, borers, flat-head
borers, leaf spot fungi, insects, mosquitoes, ants, eggs thereof,
or larva thereof.
16. A method for controlling pests, the method comprising:
obtaining a homogeneous penetrating composition comprising: at
least one active agent in a first effective amount to have an
activity of controlling a pest so as to kill, disable, and/or
immobilize the pest; and at least one biosurfactant penetrant
selected from the group of glycolipids, rhamnolipids, lipopeptides,
flavolipids, lipoproteins, phospholipids,
lipopolysaccharide-protein complexes, or
polysaccharide-protein-fatty acid complexes having the at least one
active agent in the first effective amount homogeneously dispersed
therein, the at least one biosurfactant penetrant being present in
a second effective amount for carrying the at least one active
agent in the effective amount into or through the pest in order to
control the pest, wherein the first effective amount is larger than
the second effective amount; and providing the homogeneous
penetrating composition to a pest in an amount such that the pest
is substantially controlled with the active agent.
17. The method as in claim 16, wherein the biosurfactant penetrant
is a glycolipid and the active agent is a pesticide.
18. A method for controlling pests, the method comprising:
obtaining a homogeneous penetrating composition comprising: at
least one active agent in a first effective amount to have an
activity of controlling a pest so as to kill, disable, and/or
immobilize the pest; and at least one microbial biosurfactant
penetrant obtained from a microbe and selected from the group of
glycolipids, rhamnolipids, lipopeptides, or flavolipids, having the
at least one active agent in the first effective amount
homogeneously dispersed therein, the at least one biosurfactant
penetrant being present in a second effective amount for carrying
the at least one active agent in the effective amount into or
through the pest in order to control the pest, wherein the first
effective amount is larger than the second effective amount;
providing the homogeneous penetrating composition to a pest in an
amount such that the pest is substantially controlled with the
active agent.
19. The method as in claim 18, wherein the biosurfactant is
obtained from a microbe selected from the group of: Pseudomonas
species; Flavobacterium species; Candida species; Rhodococcus
species; or Arthrobacter species.
20. The method as in claim 18, wherein the biosurfactant penetrant
is a glycolipid and the active agent is a pesticide.
Description
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a continuation of U.S. patent
application Ser. No. 11/209,132, filed on Aug. 22, 2005, which is a
continuation-in-part of U.S. patent application Ser. No.
11/141,669, filed on May 31, 2005, which claims the benefit of U.S.
Provisional Patent Application Ser. No. 60/575,913, filed Jun. 1,
2004, and benefit of U.S. Provisional Patent Application Ser. No.
60/604,139, filed Aug. 23, 2004, which patent applications are all
incorporated herein by specific reference in their entirety.
BACKGROUND OF THE INVENTION
[0002] 1. The Field of the Invention
[0003] The present invention relates to formulations that include a
penetrant. More particularly, the present invention relates to
formulations, which can be solid, liquid, or paste, and methods of
using the same for introducing active substances into plants,
humans, animals, and/or pests.
[0004] 2. The Relevant Technology
[0005] Although chemical pesticides are valuable for pest control,
their use poses many problems. They tend to harm non-target
organisms such as humans, domestic animals, beneficial insects, and
wildlife. In addition, their residues tend to remain on the crop
and may accumulate in the soil, water, or air. Another concern is
the development pesticide resistance by the targeted organisms. Due
to the serious environmental problems associated with chemical
pesticides, the demand for safer pesticides and alternate pest
control strategies is increasing.
[0006] Similarly, conventional compositions that are used for
applying, distributing, or introducing active substances (e.g.,
insecticides, herbicides, nutrients, minerals, or medicinal drugs)
into pests, insects, humans, plants, and animals, suffer from some
of the same problems. In addition, many such compositions and
compounds are expensive, difficult to handle, or are otherwise
unsuitable for some applications. Many compounds that are suitable
for use with, for example, crops, are not appropriate for use with
humans or animals. For these reasons, much of the cost of
delivering active agents relates to the costs associated with the
carriers.
[0007] Therefore, it would be advantageous to have compositions
including penetrants that can safely and effectively deliver active
substances.
SUMMARY OF THE INVENTION
[0008] Generally, embodiments of the present invention include a
homogeneous penetrating composition that can be used for increasing
the permeation of an active agent through a medium. Such a
penetrating composition can include at least one active agent. The
activity of the active agent can be beneficial for plants; or for
controlling pests. The composition also includes at least one
penetrant that is present in an effective amount for carrying the
at least one active agent into or through a medium. While the
penetrant can carry the active agent through a wide range of
mediums, the preferable mediums are plants, such as trees, soil, or
the pest's environment or habitat. As such, the penetrant with or
without an additional active agent can be used to control pests
such as insects, larvae, insect eggs, mites, algae, moss, mold,
slime, nematodes, bacteria, fungi, amoeba, mollusks, and the
like.
[0009] Additionally, the penetrant can be selected from aliphatic
sulfones, acyclic sulfones, sulfones, sulfoxides, biosurfactants,
glycolipids, lipopeptides, favolipids, polyvinylpyrrolidone,
lipoproteins, phospholipids, lipopolysaccharide-protein complexes,
polysaccharide-protein-fatty acid complexes, penetration enhancers,
and combinations thereof. The active agent can be selected from the
group consisting of pesticides, elicitors, biopesticides,
biopesticide byproducts, alkaloids, plant-growth regulators, plant
nutrients, mineral, seed treatment agents, preserving agents,
disinfectants, sterilizers, surfactants, soil conditioners, baits,
dyes, plant stress-reducing agents, and combinations thereof.
[0010] The penetrating composition can also include a solubility
controlling agent, which can either slow the release of the active
agent from the composition or increase the solubility of the active
agent within the composition. The solubility controlling agent can
be selected from the group consisting of slow release cross-linked
swellable gel, slow release cross-linked swellable polyacrylamide
gel, wax, chitin, chitosan, C12-C20 fatty acid, myristic acid,
stearic acid, palmitic acid, C12-C20 alcohol lauryl alcohol, cetyl
alcohol, myristyl alcohol, stearyl alcohol, amphiphilic esters of
fatty acids, glycerol, monoester C12-C20 fatty acids, glyceryl
monolaurate, glyceryl monopalmitate, glycerol esters of fatty
acids, polyethylene monostearate, polypropylenemonopalmitate
glycols, C12-C20 amines, lauryl amine, mystyl amine, stearyl amine,
amide C12-C20 fatty acids, and combinations thereof.
[0011] Moreover, the penetrant can form a complex with the active
agent, wherein the complex can be a chelate. The complexing
penetrant can preferably be selected from glycolipids,
lipopeptides, favolipids, lipoproteins, phospholipids,
lipopolysaccharide-protein complexes, and
polysaccharide-protein-fatty acid complexes. Additionally, the
complexed active agent can preferably be selected from a plant
nutrient, mineral, imidacloprid, acephate, phosphite salt, natural
oil, and combinations thereof.
[0012] Additionally, the penetrating composition can be used for
improving the health of a tree. As such, a method for increasing
the health of a tree can include drilling a hole into the tree, the
hole being at an angle that is not congruent with a radii of the
tree and being substantially parallel with soil from which the tree
grows. That is, the hole is not aligned or substantially aligned
with the radii, but can intersect the radii at any possible angle.
After the hole is formed, the composition is then applied into the
hole in the tree.
[0013] The composition can also be used for controlling pests,
wherein controlling a pest is considered to include killing,
disabling, or immobilizing a pests or otherwise rendering the pests
substantially incapable of causing harm. As such, the method of
controlling the pests can be performed by applying the composition
to the pest directly or indirectly. Indirect application of the
composition can be included in applying the composition to the
environment to which the pest lives, such as to a host plants,
mounds, soil, surfaces, dwellings, cracks, and the like. This can
include applications to human dwellings, office buildings, schools,
kitchens, bathrooms, bathtubs, and the like. Additionally, when an
animal is infected with a pests, such as those described herein,
the animal can be treated by spraying, coating, applying, dipping,
or other process of applying the composition to the animal. Also,
when controlling the pest, it can be preferable that the active
agent is a pesticide and/or the penetrant is a biosurfactant.
Optionally, the pesticide is complexed with the biosurfactant.
[0014] Additionally, the composition can be used for retaining
moisture in a plant. This can be done by applying the composition
to the plant, wherein the penetrant and/or active agent is a
biosurfactant. As such, the composition can be applied to any
portion of the plant, including leaves, stem, trunk, flowers,
roots, and the like. Also, the composition can be used to preserve
plant cuttings, wherein a plant cutting is a plant that have been
cultivated by being cut from the soil. The composition can preserve
the plant cutting by being applied to the plant before or after
being cut. Optionally, this can also preserve the flowers that may
be present on a plant cutting, wherein the composition can be
applied directly to the flowers, leaves, stem, or cutting site.
[0015] In one embodiment, the present invention includes a
composition for increasing the permeation of an active agent in a
mammal. Such a composition includes at least one active agent that
has an activity that is beneficial for an animal, wherein the
animal can include humans or other well-known animals. Also, the
composition includes at least one penetrant selected from the group
consisting of biosurfactants, glycolipids, lipopeptides,
favolipids, lipoproteins, phospholipids, lipopolysaccharide-protein
complexes, polysaccharide-protein-fatty acid complexes, and
combinations thereof. Preferred active agents for animals include
minerals, nutrients, vitamins, drugs, cancer drugs, and
combinations thereof. Optionally, the active agent is complexed
with the penetrant, which can be in the form of a chelate.
[0016] In one embodiment, the present invention includes a
biosurfactant composition. The biosurfactant composition can
include an effective amount of a biosurfactant for performing a
beneficial function. The beneficial function can be one of the
following: controlling a pest; preserving a plant cutting; or
reducing effects of environmental stress on a plant. Preferably,
the biosurfactant is selected from the group consisting of
glycolipids, lipoproteins, flavolipids, lipoproteins,
phospholipids, lipopolysaccharide-protein complexes,
polysaccharide-protein-fatty acid complexes, and combinations
thereof. Additionally, the further comprises a solubility
controlling agent selected from the group consisting of slow
release cross-linked swellable gel, slow release cross-linked
swellable polyacrylamide gel, aliphatic compound, wax, chitin,
chitosan, C12-C20 fatty acid, myristic acid, stearic acid, palmitic
acid, C12-C20 alcohol lauryl alcohol, cetyl alcohol, myristyl
alcohol, stearyl alcohol, amphiphilic esters of fatty acids,
glycerol, monoester C12-C20 fatty acids, glyceryl monolaurate,
glyceryl monopalmitate, glycerol esters of fatty acids,
polyethylene monostearate, polypropylenemonopalmitate glycols,
C12-C20 amines, lauryl amine, mystyl amine, stearyl amine, amide
C12-C20 fatty acids, and combinations thereof.
[0017] In the instance the biosurfactant composition is used for
controlling pests, the composition further comprises at least one
active agent in an effective amount for controlling pests, the at
least one active agent being selected from the group consisting of
pesticides, insecticides, sterilants, disinfectants, miticides,
fungicides, bactericides, viricides, mollucides, nematicides,
algicides, herbicides, and combinations thereof. Also, the method
of controlling the pests can include applying the biosurfactant
composition to a pest. This can include being applied to the
environment in which the pests lives, such as an ant mound, to
protect plants, soils, aquatic systems, ponds, homes, or structures
such as kitchens, bathrooms, or bathtub surfaces. As such, the
active agent along with the penetrant can be applied when in the
form of a gel, solid capsule, or tablets, especially for ant mound
treatments.
[0018] In the instance the biosurfactant composition is used for
reducing effects of environmental stress on a plant the composition
can be applied to any portion of the plant. This can also include
applying the biosurfactant composition to the soil surrounding or
proximate to the plant. Also, the bio surfactantcomposition can be
used to preserve a plant that has been cultivated by being cut. As
such, the composition can be applied to a plant before or after
being cut, such as contacting the biosurfactant to the site where
the plant was cut. Optionally, a plant cutting that includes a
flower can be preserved, which can include applying the
biosurfactant to the flower.
[0019] Additionally, the biosurfactant composition can be
configured to have a slow rate of release, which may be a
zero-order kinetic rate of release. In any event, by including a
solubility controlling agent in the biosurfactant composition, the
rate at which the biosurfactant is released from the composition
can be controlled and at a slower rate. As such, applying the
biosurfactant composition to a medium can slowly release the
biosurfactant to penetrate the medium, wherein the medium is at
least one of a plant or pest. While the solubility controlling
agent can be any of such agents described herein, it is preferable
that the agent is a cross-linked swellable polyacrylamide gel.
BRIEF DESCRIPTION OF THE DRAWINGS
[0020] To further clarify the advantages and features of the
present invention, a more particular description of the invention
will be rendered by reference to specific embodiments thereof which
are illustrated in the appended drawings. It is appreciated that
these drawings depict only typical embodiments of the invention and
are therefore not to be considered limiting of its scope. The
invention will be described and explained with additional
specificity and detail through the use of the accompanying drawings
in which:
[0021] FIG. 1 illustrates examples of six different structure of
rhamnose lipids R1, R2, R3, F4, A and B of Pseudomonas
aeruginosa;
[0022] FIG. 2A illustrates a prior art method of embedding a
capsule, such as those disclosed herein, into a tree; and
[0023] FIGS. 2B-2C illustrate a novel method of embedding a
capsule, such as those disclosed herein, into a tree.
DETAILED DESCRIPTION OF EMBODIMENTS OF THE INVENTION
[0024] Generally, embodiments of the present invention relate to
compositions that can be used for treating plants and methods of
using the same. The compositions include at least one penetrant or
carrier and at least one active substance, e.g., pesticides. The
penetrant can be used as a carrier of active substances to enhance
the solubility, complexation, permeability, wettability and/or
translocation of active substances to and within plants, seeds, and
into soils and pests. Optionally, the compositions may also include
one or more solubility controlling agents and additives.
[0025] Penetrating compounds can be used for treating trees in
order to obtain many desirable results. In part, the benefits can
be due to the ability of the dissolved solution to penetrate deeply
and efficiently into the treated body, and to penetrate the
conductive vascular tissue, the non-conductive tissues, and
heartwood of the tree. Consequently, fewer holes may need to be
drilled around the tree perimeter. The ability to treat trees,
while drilling fewer holes than those that generally have been
required in conventional treatments, is highly advantageous because
it can minimize the risks of infections that may occur from decay,
adverse organisms, or secondary infections by insects.
[0026] In one embodiment of the invention, formulations are
prepared to include penetrants configured to be absorbed into
seeds, trees, plants, pests, soils, and the like. As such, these
penetrant-containing formulations can be used in applications to
treat seeds, plants, pests and soils as described herein and in the
incorporated references.
[0027] In another embodiment of the invention, formulations are
prepared to enhance penetration and increase the radial and
tangential flow of active agents through the treated plant. It can
be preferable to use semi-solid or solid preparations for tree
injections or soil applications. This can be especially important
to enhance the lateral and radial diffusion and/or penetration of
the injection material.
[0028] In another embodiment of the invention, aliphatic and
acyclic sulfones can be used as carriers and penetrants in tree
and/or plant treatment formulations. Examples of the sulfones are
Methylsulfonylmethane (MSM), ethyl sulfone, butadiene sulfone. MSM
can be preferable in some applications because of the many
advantages that are explained in more detail below. Thus, the
aliphatic and acyclic sulfones can be used as a carrier, adjuvant,
surfactant, and/or penetrant for active substances.
[0029] Additionally, formulations using MSM and other sulfones may
be used for applications to treat seeds, plants, pests and soils.
Accordingly, the formulations can be prepared as solid, semi-solid,
powders, gels, pastes, liquids, and the like. Moreover, MSM and/or
the other sulfones may be used as a matrix base for different types
of formulations (solid, semi-solid, paste, gel, cream, or liquid).
For example, a solid pesticidal tablet, which includes MSM or other
sulfone can be a carrier or penetrant.
[0030] Methylsulfonylmethane is a chemical with many favorable
characteristics. It is a natural, safe, inexpensive, small
molecule, and is stable at high temperatures with a melting point
(mp) of 109.degree. C., and boiling point (bp.sub.760) of
238.degree. C. Its non-hygroscopic nature, solvent action, and
moderate melting point make it ideal for solid preparations such as
tablets. Merck's Index describes it as being a high temperature
solvent for many inorganic and organic compounds. Additionally, the
other sulfones have similar favorable characteristics.
[0031] Research and data show that MSM and/or other sulfones can be
effective penetrants with many useful functions, such as
permeability, wetting agent, mobility, and a translocation enhancer
of many active substances through dead or live tissues of plants
and pests, and can be a very effective solubilizer of substances.
MSM and/or other sulfones have many advantages over the well-known
penetrants used in the pharmaceutical industry. In addition to the
favorable characteristics mentioned above, MSM has a low molecular
weight, non-toxicity, and/or in a solid state at room temperature,
which is ideal for use in solid formulations as a carrier,
translocation enhancer, and/or a stabilizer in formulations.
[0032] MSM can be a good binding agent for tabletting. As such, it
can be used as a sole carrier and excipient in tabletting and
molding. Its ideal melting point of 109.degree. C. makes it an
excellent carrier and solvent for water insoluble substances and
active agents, (e.g., pesticides). Its binding ability without the
addition of excipients makes it a good carrier of heat sensitive
active substances in tabletting formulations. Additionally, testing
MSM in tree injections at a 100% concentration did not induce any
toxicity or necrosis for the treated plants. Thus, MSM and/or other
sulfones can be valuable in treating plants without inducing
toxicity or necrosis.
[0033] In another embodiment of the invention, biosurfactants can
be used as carriers and penetrants of active agents, such as
insecticides, herbicides, nutrients and minerals, medicinal drugs
for humans and animals, and on the like. Microbial biosurfactants
are compounds produced by variety of microorganisms such as
bacteria, fungi, and yeast. Biosurfactants include
low-molecular-weight glycolipids (GLs), lipopeptides (LPs),
flavolipids (FLs), and high-molecular-weight polymers such as
lipoproteins, lipopolysaccharide-protein complexes, and
polysaccharide-protein-fatty acid complexes. Glycolipids,
flavolipids, and lipopeptides form an important class of secondary
metabolites that occur in many microorganisms such as Pseudomonas
species (P. aeruginosa, P. putida, P. florescens, P. fragi, P.
syringae), Flavobacterium spp., Bacillus spp. (B. subtilis, B.
pumillus, B. cereus, B. licheniformis), Candida species (C.
albicans, C. rugosa, C. tropicalis, C. lipolytica, C. torulopsis),
Rhodococcus sp.; Arthrobacter spp., and on the like.
[0034] Biosurfactants have a great deal of structural diversity.
Biogenetically, GLs, FLs, and LPs are derived from fatty acids that
are linked either to sugars, organic acid, or peptides,
respectively. For example, rhamnolipids are produced by different
Pseudomonas bacterial strains and they constitute a subset of the
glycolipids where one or two rhamnose sugars are attached to one or
more fatty acids having a saturated or unsaturated alkyl chain.
Some strains produce monorhamnolipid (R1) or dirhamnolipid (R2),
others produce a mixture of R1 and R2 or different structural
homologs of rhamnolipids, and some strains do not produce
rhamnolipids. There are at least six forms of rhamnolipids
described in the literature. A single form or a mixture of the
different forms of rhamnolipids may be used to achieve the
objectives of the invention.
[0035] FIG. 1 depicts six different rhamnolipids, which can be used
in accordance with the present invention. R1 is an alpha-L
rhamnopyranosyl-Beta-hydroxydeconyl-Beta-hydroxydecanoate. R2 is a
2-O-alpha-L-rhamnopyranosyl-alpha-L-rhamnopyranosyl-Beta.
[0036] FIG. 1 illustrates examples of different structures of
rhamnose lipids. The rhamnose lipid "R1" is an
alpha-L-rhamnopyranosyl-beta-hydroxydeconyl-beta-hydroxydecanoate.
The rhamnose lipid "R2" is a
2-O-alpha-L-rhamnopyranosyl-alpha-L-rhamnopyranosyl-beta-hydroxydeconyl-b-
eta-hydroxydecanoate. The rhamnose lipid "R3" is an
alpha-L-rhamnopyranosyl-beta-hydroxydeconic acid. The rhamnose
lipid "R4" is a
2-O-alpha-L-rhamnopyranosyl-alpha-L-rhamnopyranosyl-beta-hydroxydeca-
noic acid. The rhamnose lipid "A" is a
2-O-alpha-decenoyl-alpha-L-rhamnopyranosyl-beta-hydroxydeconyl-beta-hydro-
xydecanoic acid. The rhamnose lipid "B" is
2-O-(2-O-alpha-decenoyl-alpha-L-rhamnopyranosyl)-alpha-L-rhamnopyrano
syl-beta-hydroxydeconyl-beta-hydroxydecanoic acid. While these
rhamnose lipids have been depicted and described, other rhamanose
lipids can also be used in the present invention.
[0037] In one embodiment, a single biosurfactant or a mixture of
different biosurfactants may be used as penetrants or carriers in a
formulation that can perform the functions and achieve the results
described herein. In another embodiment, the aforementioned
compounds may also be synthesized by standard organic synthesis
methods.
[0038] Rhamnolipids may be used as a matrix base or carrier in
different types of formulations (solid, semi-solid, paste, gel, or
liquid) for plant and tree treatments. Preliminary research and
data show that rhamnolipids can be effective carriers through plant
tissues, having many useful functions such as permeability, wetting
agent, mobility, and a translocation enhancer of many active
substances through plants. It is also an effective
solubility-controlling agent of many substances. For instance,
addition of the rhamnolipid to a water-soluble insecticide acephate
formulation helps control the solubility in order to provide the
insecticide at a predetermined rate. Combining the rhamnolipid with
the water insoluble insecticide imidacloprid helps enhances the
solubility as well as the translocation of the insecticide into the
treated plant or tree. Moreover, solid and/or semisolid rhamnolipid
formulations can be used as a penetrant and/or as a fungicide to
treat trees for fungal diseases.
[0039] Co-pending patent application Ser. No. 11/141,669, filed May
31, 2005, is incorporated herein by reference and describes
biosurfactants (e.g. GLs, FLs, and LPs etc) having a powerful
biopesticidal activity against many pests and diseases that affect
plants. These biosurfactants also have similar biopesticide
activity against pests and diseases affecting humans and animals.
The pests that can be controlled by biosurfactants include insects,
insect larvae and eggs, mites, algae (e.g. seaweeds, pond algae,
and the microscopic algae such as blue-green algae), microbial
pests (e.g. nematodes, bacteria, fungi, amoeba, parasites, etc.),
moss, slime, lichens, mold, mollusks, and plant weeds. In addition,
these biosurfactants may be used to treat human diseases such as
ova-parasites, cysts, athlete foot and nail fungi infections, yeast
infection, and hair dandruff, and the like. Biosurfactants may also
be used in human chelation therapy and reduction of heavy metal
toxicity. This makes these biosurfactants very effective carriers,
penetrants, and biopesticides, with a wide range of beneficial
uses. For example, rhamnolipids have been shown to be effective
against dandruff, and as spermicidal agent.
[0040] In another embodiment, MSM or dimethyl sulfoxide (DMSO) is
combined with a biosurfactant (e.g., rhamnolipid) to enhance the
permeability and translocation of the carried active agents, (e.g.,
dyes or insecticides). Consequently, the effectiveness of the
carried compound or active agent, as well as the fungicidal
activity of the rhamnolipid is enhanced. It is thought, without
being bound thereto, that a synergistic effect may exist between
some combinations of the foregoing compounds. Tests of pesticidal
formulations using high amounts of DMSO in solid or semisolid
preparations show no toxicity or necrotic symptoms on the treated
plants. The use of DMSO enhances penetration and effectiveness of
the active agents such as insecticides.
[0041] Another advantage of using rhamnolipids, MSM, and/or DMSO as
a carrier in plant and tree treatments is their antimicrobial
activity. This can be very beneficial in tree injection
applications where the method of application causes injury to the
roots or the trunk. Many wood-decay and rot causing organisms can
be found in soil or on tree trunks. These harmful organisms may
propagate and grow at the injection site and within the vascular
tissue of the treated tree. This may block the vascular system and
cause the eventual death of the treated tree. Rhamnolipids, MSM,
and/or DMSO have biocidal activities that can be used in tree
injection formulations in order to inhibit the growth of many
adverse organisms. This is essential for the treated plant to have
a fast recovery and can eliminate the need of disinfecting the
drill bit with alcohol or flame after each treatment.
[0042] Additionally, antimicrobial agents such as fungicides,
bactericides, and preservatives may be included in formulations
where the penetrant has no antimicrobial activity. This may be
beneficial for some tree injection applications. Of course, the
antimicrobial agents could be used with penetrants that have
antimicrobial activity.
[0043] In another embodiment of the invention, biosurfactants
glycolipids, flavolipids, and/or lipopeptides can be used as
complexing/chelating agent and/or delivery agents for plant
nutrients. Treatment of nutrient deficiencies can be greatly
advanced by a method that not only solubilizes metals but also
facilitates the introduction of these metals across the
wall/membrane barriers. The use of metal delivery agents can be a
beneficial method of treatment to combat nutrient deficiencies in
plants, but it also can be the most challenging for three reasons:
(1) the metal of interest has to be encapsulated or chelated within
the delivery agent; (2) the metal complexes must penetrate a large
number of plant cells and/or the hydrophobic leaf cuticle; and (3)
the metal and/or delivery agents must be safe to the plant and the
environment over the time of treatment. Accordingly, the following
qualities of the present invention help to address these
issues.
[0044] It has been shown that encapsulation of active agents with
glycolipids such as rhamnolipids have enhanced stability constants
over other organic acids. This is probably due to the fact that
these biomolecules chelate or complex with metals more efficiently
through the carboxyl group on the fatty acid moiety and the
hydroxyl groups on the rhamnose. However, encapsulation and
solubility alone may not be sufficient criteria for improved
bioavailability, but penetration can improve bioavailability. A
neutral metal-ligand complex that has an enhanced binding affinity
towards the cell membrane through the hydrophobic fatty acid moiety
can facilitate fusion with the cell membrane. This allows the
complex to enter the cell via endocytosis. After endosomal release,
the metal becomes readily available within the cytoplasm.
Additionally, glycolipids, flavolipids, and/or lipopeptides are
biological molecules that are environmentally safe, unlike many
other synthetic chelating agents.
[0045] In another embodiment, the present invention is readily
adaptable to a more general modular delivery system, where each
modular component can provide a key step of metal delivery into
plants. Such an approach can have two major components: (1) a
chelating moiety to help chelate the metal ions; and (2) a lipid
moiety to enhance absorption. The end result can be a system that
chelates metals and penetrates through the cellular barriers to
achieve the ultimate treatment for metal deficiency. As described
herein, GLs, FLs and LPs can serve as carriers for various
nutrients across the membranes of plant cells or leaf tissues.
[0046] In one embodiment, the penetrants and carriers of the
present invention can increase the solubility of various agents to
enable increase homogenous distribution throughout the treated
plants and soils. Also, the penetrants and carriers can protect the
metal from antagonists present in nature and from changes in the
pH, which provides for much greater stability. The enhanced
absorption of the metal-GL, metal-FL and/or metal-LP complexes can
be more absorbable than the inorganic or un-complexed form of the
metal. This is the result of two synergetic effects: (a) the ligand
neutralizes the charge of the inorganic metal, and (b) the ligand
serves as a permeation agent through its hydrophobic fatty acid
moiety. The present invention can also reduce the interaction and
binding of the chelated metal with adverse antagonists, which
improves uptake and decreases elimination, so as to provide
improved utilization. Moreover, the formulations have improved
safety towards plants and the environment by being totally
natural.
[0047] Of particular interest is a new class of flavolipids
biosurfactants that feature citric acid as a polar moiety.
Flavolipids, like other microbial-produced surfactants, exist in
different forms or structural homologs. There are at least
thirty-seven known flavolipid homologs produced by flavobacterium
genus (Bodour et al. 2004). Flavolipids are very likely to exhibit
a higher stability constant with some metals (e.g., iron) due to
being similar with the iron chelators arthrobactin and aerobactin.
Due to the many different biosurfactant types and structural
homologs, the choice of the biosurfactant-metal complex can be
determined based on the stability constant of the complex. Thus,
different ratios of the biosurfactants to the nutrients may be
used.
[0048] As a result, the present invention employs biosurfactants,
such as glycolipids, flavolipids, lipopeptides, and the like, as
well as a mixture thereof as nutrients complexing/delivery agents
to maintain the nutrients in a soluble, usable form for the plant.
Preliminary tests using mono- and di-rhamnolipids provide stable
complexes with different nutrients such as Zn, Fe, Cu, NH.sub.4,
Ca, and K. The use of rhamnolipid in formulations containing iron
can inhibit the oxidation of iron to the unavailable oxide forms,
and eliminates staining associated with iron fertilizers,
especially for the home and garden market For example, derivatives
of the foregoing compounds or biosurfactants having similar
characteristics, having a non-polar moiety (hydrophobic), having a
polar moiety (hydrophilic), and/or being able to complex,
solubilize or enhance the uptake of active agents (e.g., plant
nutrients and insecticides) may also be employed.
[0049] In another embodiment of the invention, biosurfactants may
be used as solubility controlling agents for active compounds.
Biosurfactants may also be used to coat plant fertilizers, such as
urea, ammonium nitrate, potassium nitrate, ammonium phosphate,
ferrous sulfate, and the like, and reduce their solubility and
transformation in the soil. The antimicrobial activity of some
biosurfactants such as rhamnolipids may inhibit the activity of
many degrading microorganisms and may reduce the transformation
rate of the treated fertilizer. The addition of other solubility
controlling agents described in this invention (e.g., C12-C20 fatty
acids) to the formulations may also be desired. In addition to
coating active agents, the presence of the biosurfactant in the
formulations can aid in penetration and complexation of the carried
agents.
[0050] In one embodiment of the invention, GLs, FLs, and/or LPs
plant nutrient compositions may be applied to the plants or soil in
solution, solid, and semi-solid compositions and in different
shapes and forms. An alternate method of application involves
adding the GLs, FLs, or LPs, which can be with or without plant
nutrients, to the soil or the growing media (e.g., hydroponics,
potting soil mix, soil-less medium) where crops are grown or to be
grown. The added GLs, FLs, and LPs can solubilize and complex
nutrients that are in the soil and make them available to the
plants. However, it is preferable to use the pre-formulated
biosurfactant-nutrient complex as described herein. The GLs, FLs,
and/or LPs can be used as soil penetrants to maintain nutrients in
solution and enhance their uptake by the plants. In this
embodiment, soil structure may be improved, and the cation exchange
capacity (CEC) of the soil may be raised. Enhancement of CEC is
very beneficial for sandy soils (e.g., golf courses) to maintain
the nutrients in the root zone and to reduce pollution, waste, and
leaching of nutrients.
[0051] GLs, FLs, and/or LPs producing organisms (e.g., rhamnolipids
producing Pseudomonas spp.) can be added to the soil or the growing
media. These organisms can grow and produce the biosurfactants that
complex and make nutrients available for the growing plants. The
produced biosurfactants may also help the active agents penetrate
through the roots. The cultures may be mixed with growth
enhancement substances, such as oils, sugar or other compounds, to
aid in their growth.
[0052] In another embodiment of the invention, the GLs, FLs, LPs or
a mixture as penetrants and complexing agents can be added to
pre-formulated fertilizer products (chelated and non-chelated) to
enhance nutrients uptake.
[0053] In another embodiment of the invention, the GLs, FLs, LPs,
and/or mixture thereof may be combined with other chelating agents
(synthetic or natural) used in the fields of plant, human, or
animal nutrition. In one embodiment, natural chelating agents are
used. Although not necessary, a chelating agent is used that has
metal-conditional stability constant similar to or less than the
conditional stability constant of GLs-FLs, or LPs-metal complexes.
The presence of the GLs, FLs, or LPs in the composition can help in
the penetration of the complexed nutrients as described in the
invention.
[0054] Using GLs, FLs or LPs as complexing agents for nutrients may
also be beneficial for foliar application. In minute amounts (100
ppm or less), biosurfactants have a natural tendency to lower the
surface tension of the applied mixture, which reduces or eliminates
the need for adding surfactants before spraying plant leaves. In
general, foliar application of agrochemicals active agents can be
associated with quick dryness on the leaf surface and poor uptake
of the active agents. Salt accumulation on the leaf surface is
sometimes noticeable within few minutes of foliar application. The
presence of the fatty acid moiety in the biosurfactants maintains
the applied active agents with or without a matrix in a hydrated
form for a longer period of time and effectively improves the
uptake and permeability of the carried active agents through the
leaf. Preliminary results show that the uptake of the active agent
was directly related with the concentration of the biosurfactant.
At biosurfactant concentrations of about 500 ppm and above, the
uptake of the carried active agents, especially nutrients, is
greatly increased.
[0055] The presence of the lipid moiety in the biosurfactants acts
as a barrier or insulator on the leaves and may aid in maintaining
the cells hydrated. This helps reduce moisture loss and
evapo-transpiration from the sprayed leaves, this can have the
potential of reducing water consumption in the treated plants to
aid in conserving water. Furthermore, the biosurfactants can be
used for the prevention and protection of treated plants against
environmental stress conditions such as drought and frost.
[0056] In another embodiment, flavolipids can be used as a source
of organic nitrogen as a nutrient to supply plants with this
nutrient. Also, the biosurfactants can be used as preservatives for
flower and plant cuttings.
[0057] Other penetrants that may be used in the invention are
penetrants used in the pharmaceutical industry as tissue softening
agents, as carriers of medicaments, and as gene transfer agents.
Examples of penetration enhancers include: alcohols, such as
ethanol, isopropanol, and methanol; polyols, such as n-alkanols,
myoinositol, pinitol, limonene, terpenes, dioxolane, propylene
glycol, ethylene glycol, and glycerol; acyclic polyols such as
mannitol, sorbitol, and xylitol; alkyl methyl sulfoxides, such as
decylmethyl sulfoxide, dimethyl sulfoxide, tetradecyl methyl
sulfoxide; esters, such as isopropyl myristate/palmitate, ethyl
acetate, butyl acetate, methyl propionate, capric/caprylic
triglycerides; ketones; amides, such as sulfamides, acetamides,
acetamide oleates; various surfactants, such as sodium lauryl
sulfate, quaternary ammonium salts, lecithins, cephalins,
alkylbetamines; various alkanoic acids such as caprylic acid;
lactam compounds, such as laurocapram; alkanols, such as cetyl
alcohol, oleyl alcohol, stearyl alcohol; and miscellaneous
compounds as dimethyl acetamide, dimethyl formamide, and
N,N-diethyl-m-toluamide, tetrahydrofurfuryl alcohol, dialkylamino
acetates, and pyrrolidones (2-pyrrolidone, N-methyl-2-pyrrolidone,
N-(2-Hydroxyethyl) pyrrolidone, and sorbitan. Another set of
penetrating agents used in the pharmaceutical industry are gene
transfer agents that introduce genes and active compounds through
the cell membrane. Typically, these agents modify the charge on the
membrane, and thereby allow the charged molecule to enter through
the membrane. Example of these gene transfer agent are: bile salts,
poly(acids), poly(bases), glycerophosphates or their salts,
steroidal polyamines, and the like.
[0058] Combinations of the liquid penetrants glycerol, propylene
glycol, and DMSO with additives or gelling agents such as
polysaccharides (starch, cellulose), chitin, pectin, alginate
salts, polyethylene glycol, or stearate derivatives, may be
formulated to make solid or semi-solid formulations such as gel,
paste, spikes, blocks, tablets, or rods for soil, root, or trunk
application. While being used as carriers in tree injection
treatments, the physical state of penetrants may be liquid, solid,
or semi-solid. Penetrants may also have solvent action.
Additionally, poly(acids), poly(bases), or glycerophosphates can be
made in a paste form. For example, combining Poly(lactide) with
calcium salts forms semi-solid preparation that can change into
solid.
[0059] Additionally, the solubilizing agent ethanolamines such as
tri-ethanolamine and its salts (sulfates, phosphates, salicylates,
and HCl) are also effective penetrants through wood and plant
tissues. These may be used to make solid or liquid preparations
that can be used as carriers for active agents, especially for tree
injection compositions.
[0060] Accordingly, there are no specific limitations as to the
kind of penetrant to be used, as long as it is capable of carrying
active agents, and if necessary, solubilize the active agents to be
easily absorbed or translocated by plant tissues. If necessary, a
solvent may be added to the penetrating agent to help in the
solubilization of hard-to-dissolve compounds in a certain
penetrant. For example, mannitol, sorbitol, ammonium ion, and/or
urea have some penetration capability, but limited solvent
activity. The addition of a solubilizer, such as polyethylene
gylcol or polyethylene oxide, may enhance their activity.
[0061] In tree injection applications, naturally solid penetrants
may be used, and/or penetrants may be prepared in solid or
semi-solid (e.g., gel, paste, cream) formulations using carriers
and penetrants with solvent action and having a low molecular
weight. The presence of a penetrant-solvent in the semisolid or
solid formulations is helpful in delaying the formation of a callus
layer (resin) at the site of the treatment injection. Many trees,
such as conifers, peaches, and apricots, tend to produce and
accumulate excessive resin after injury. The solid tree injection
formulations of the present invention having penetrants DMSO, MSM,
rhamnolipids, and/or triethanolamine can delay the accumulation of
resin till the formulation is substantially dissolved and used by
the treated plant.
[0062] Additionally, the penetrating agent can enhance the
permeability of the carried active component through treated plant
roots. By placing the treatment compound next to the root,
permeability is significantly improved and better uptake of the
active component by the plants is achieved. Better uptake of the
active component by plants with the aid of a penetrant reduces the
possibility of waste and minimizes contaminating the environment.
By increasing absorption efficiency and translocation in the
plants, soil fixation or leaching of the active compounds is
reduced.
[0063] Treating an individual plant through root flares and/or
trunk injections can enable the penetrating agent to improve
vertical, horizontal, and/or radial penetration, as well as the
tangential flow of the carried material. As such, better
distribution of the active compound in the treated plant can be
achieved. In the case of treating against borer insects, better
penetration and distribution of the active agent can be essential
for the success of the overall therapy. This is especially
important for the insecticidal treatment against borers (e.g.,
Aspen borers) that tunnel deeply into the heartwood of the stem,
where the activity of the vascular tree sap is minimal and the
treating agent has minimal access. The presence of a penetrant,
such as DMSO, MSM, and/or triethanolamine, in the insecticidal
formulation can facilitate the penetration of the insecticide
toward the heartwood of the treated trunk and significantly
increases the success rate of borers control.
[0064] In the instance of treating trees, it is not necessary to
drill holes and inject the formulations at equally spaced intervals
around the circumference of the tree. Instead, the presence of a
penetrant helps the injected material flow horizontally and
vertically through the trunk and root flares. Due to the increase
in the horizontal and/or vertical flow, the same size tree may be
treated with fewer injections than would otherwise be needed. Fewer
injections mean fewer holes need to be drilled and, advantageously,
at wider spacing intervals between the injections. Depending on the
amount of material that is injected, the lateral movement can
ultimately lead to the development of a complete ring of the
injected material diffusing through the trunk.
[0065] In one embodiment, the penetrants and carriers of the
present invention can be used to treat seeds. As such, a penetrant
may also be incorporated with seed treatment agents. The
formulations can be mixed with the seeds, or incorporated into seed
coating formulations.
[0066] In another embodiment, a controlled release formulation can
be prepared to include a matrix of the penetrant and/or carrier
having an active compound dissolved or dispersed therein This
allows the active compound to be released over time. As such, it is
possible to achieve superior control over the dissolution rate of
the solid or semi-solid compositions so they can be used in a
variety of applications. This can be especially essential for root
flare or trunk injection techniques in order to control the release
rate of the active agent, and/or to enhance the radial and lateral
flow of injected material. Enhancement of lateral and radial
transport can provide effective distribution of the active agents,
and fewer holes may need to be drilled around the tree. Controlled
release formulas may be used for compounds that are phyto-toxic for
plants and also to be used for formulations having active agents
with short half-lifes.
[0067] A controlled release matrix can be formed from a composition
including a carrier with or without a penetrant and a solubility
control agent. Solubility control agents may include amphiphilic
compounds having a hydrophilic portion and a hydrophobic portion,
which are usually located at opposite ends of the molecule. The
presence of hydrophobic portions in the solubility control agent
can slow down the rate at which the matrix is dissolved or eroded
when in contact with tree sap or a liquid environment. The use of a
large amount of hydrophobic component in the formulation can
greatly retard solubility of the formulation. Therefore, the
release kinetics of the active ingredient can be determined by the
properties of the matrix components. In addition, the shape of the
formulation may affect solubility. Accordingly, varying the size
and shape of the formulation as well as the proportion of the
solubility--controlling agent can control the rate of dissolution.
Also, the process of formulation may affect the solubility of the
matrix. For instance, the pressure applied by a tablet press during
the manufacturing process can be adjusted to determine the
solubility of the dosage. Exerting more pressure produces stiffer
tablets that take longer to dissolve when used to treat trees.
[0068] In another embodiment, solubility control agents or
excipients may be used in the formulations to control the release
of the active substances. Suitable solubility control agents may
include the following: wax; chitin; chitosan; C12-C20 fatty acids
such as myristic acid, stearic acid, palmitic acid; C12-C20
alcohols such as lauryl alcohol, cetyl alcohol, myristyl alcohol,
and stearyl alcohol; amphiphilic esters of fatty acids with
glycerol; monoesters; C12-C20 fatty acids such as glyceryl
monolaurate, glyceryl monopalmitate; glycol esters of fatty acids
such as polyethylene monostearate or polypropylenemonopalmitate
glycols; C12-C20 amines such as lauryl amine, myristyl amine,
stearyl amine; and amides C12-C20 fatty acids. Additional
ingredients can be incorporated in the formulation to modify the
properties of the composition and to improve the compatibility
between the components.
[0069] The agro-chemically active substances that can be used in
the present formulations are to be understood as all substances
which are customarily used for the treatment of plants Accordingly,
the agro-chemically active substances can include the following:
pesticides which include insecticides, miticides, fungicides,
bactericides, viricides, mollucides, nematicides, algicides, mos
sicides, and herbicides; elicitors, plant activators, or substances
that may enhance the defense mechanism of the plant such as
acibenzolar-5-methyl, azadirachtin, phosphorous acid or phosphite
salts, and the like; biopesticides such as pseudomonas spp,
Bacillus thurengesis, Trichoderma spp, bacteriophages, etc;
biopesticides byproducts; plants or herbal alkaloids and extracts
with insecticidal activity such as garlic, pepper, tomato, neem,
matrine, oxymatrine extracts, etc; plant-growth regulators such as
auxins, gibberellins, cytokinins, ethephon, and chlorocholine
chloride; organic and inorganic plant nutrients to provide plants
with essential nutrients such as nitrogen, phosphorus, potassium,
calcium, magnesium, sulfur, iron, zinc, manganese, etc; seed
treatment agents; flowers and ornamental cuttings; shelf-life
extending agents or preserving agents such as 8-hydroxyquinoline
citrate, citric acid, sucrose, and the like; surfactants; soil
conditioners; baits; florescent and non-florescent dyes for flowers
and ornamental cuttings and for plants; and plant stress reducing
agents such as anti-frost and drought resistant agents.
[0070] Suitable additives, which may be contained in the
plant-treatment compositions can be substances customarily used for
such preparations. Examples of such additives include adjuvants,
surfactants, emulsifying agents, sticker, buffering agents, pH
adjusting agents, fillers, plasticizers, lubricants, glidants,
colorants, pigments, bittering agents, preservatives, stabilizers,
and ultra-violet light resistant agents. Stiffening or hardening
agents may also be incorporated to strengthen the formulations and
make them strong enough to resist pressure or force in certain
applications.
[0071] Examples of buffering agents include organic acids, amino
acids, their salts, or a mixture thereof. Suitable buffering agents
include acetate, arginine, aspartate, citrate, tartarate, malate,
lactic acid, oxalate, malonate, glucoheptonate, pyruvate,
galactarate, glucarate, gluconate, tartronate, glutamate, glycine,
lysine, glutamine, methionine, cysteine, and a mixture thereof.
Phosphoric and phosphorous acids or their salts and derivatives
(polyphosphates or polyphosphites) may also be used. Synthetic
buffers are suitable to be used but it is preferable to use organic
and amino acids buffers. In addition to their buffering capacity,
some of these listed compounds may help in the chelation or
complexation of plant metals. The presence of the GLs, FLs, or LPs
in the composition can help in the penetration of the complexed
nutrients as described in the invention.
[0072] Methods of carrying out the therapeutic processes in
accordance to the invention can provide formulations with the
desired amount of the components. As such, the components are mixed
with one another and heated, if desired, while being stirred or
kneaded. The active compound can be incorporated into the penetrant
matrix by being mixed directly in the matrix, dissolved in a molten
matrix, or dispersed and mixed into the matrix. The ratio of active
compound to matrix may vary within wide limits. The final product
of the invention can be prepared by conventional procedures such as
compression molding, tabletting, pressing, extrusion, injection
molding, and preparing a solution.
[0073] Solid formulations may have different forms and shapes such
as cylinders, rods, blocks, capsules, tablets, pills, pellets,
strips, spikes, and/or the like. Solid formulations may also be
milled, granulated, or powdered. The granulated or powdered
material may be pressed into tablets or used to fill
pre-manufactured gelatin capsules or shells. Solidified penetrants
or complexing agents, such as MSM or glycolipids may be combined
with the desired active agent, such as pesticides or nutrients.
These formulations may be applied to a tree as is or reconstituted
into a liquid format prior to use. Semi solid formulations can be
prepared in paste, wax, suppository, gel, or cream preparations.
Liquid formulations can be prepared in aqueous or any other desired
solvent medium.
[0074] The formulations can be encapsulated using components known
in the pharmaceutical industry. Encapsulation can protect the
components from undesirable reactions and help the ingredients
resist adverse conditions in the environment or the treated object
or body (e.g., stomach). For human or animal applications, the
formulations may be prepared in liquid, paste, ointment,
suppository, capsule, tablet, or other well-known forms, and used
in a way similar to drugs used in the medicinal drugs industry.
Additionally, the compositions according to the invention can be
applied to the plants, pests, or soil using various methods of
application. Each method of application may be preferred under
certain circumstances.
[0075] In one embodiment, the compositions in accordance with the
invention may be used to introduce the active compounds into the
soil or the target site such as an ant mound. Also, these
preparations can be incorporated into the soil in the vicinity of
the roots of the plants, in the form of a liquid, bait, powder,
dusting, or granules. Alternatively, they are inserted in the soil
as tablets, spikes, rods, or other shaped moldings. It can be more
desirable to use tablets, rods, or spikes to minimize the
reactivity and fixation of the active agents with soil particles.
This can be important for pesticides, in particular, since their
organic nature tend to be more reactive with soil particles. The
action of the penetrant can help reduce pesticides-soil particle
interactions by maintaining the pesticide in a soluble form to
enhance penetration through root cells.
[0076] In one embodiment, the compositions can be used for treating
individual trees or plants. For example, the formulations can be
molded in different shapes or forms (e.g., solid, paste or gel, or
liquid) and introduced into the vascular tissue of the plants. The
molding can be in the form of tablets, capsules, plugs, rods,
spikes, films, strips, nails, or plates. The shaped moldings can be
introduced into holes pre-drilled in the plants or root flares, or
they can be pushed or punched into the cambium layer.
[0077] One method of applying or using the compositions of the
invention is to use dispensing devices, such as syringes, pumps or
caulk guns, paste-tubes or plunger tubes for delivering semi-solid
formulations (e.g., paste, gel, cream), into drilled holes in tree
trunks or root flares. This method may be used for formulations
that may or may not include penetrants.
[0078] Also, the compositions can be applied in the form of paste,
gel, coating, strip, or plaster onto the surface of the plant. In
one method, a plaster or strip may have a semi-solid formulation
with the insecticide being placed on the side that will contact the
tree, bush, or rose during the treatment. The same strip may have
glue or adhesive at one or both ends to wrap around or stick to the
subject being treated. Alternatively, the active agent can be
combined with the adhesive over any portion of the strip.
[0079] The compositions can also be sprayed or dusted on the leaves
in the form of pellets, spray solution, granules, or dust.
Ingredients concentrations in the sprayable or dusting, as well as
the formulations application rate may be varied widely depending on
the active agents used and/or the plants being treated.
[0080] The solid or semi-solid compositions can be coated onto
tablets using film-coating compounds well-known in the
pharmaceutical industry such as polyethylene glycol, gelatin,
sorbitol, gum, sugar, or polyvinyl alcohol. This is particularly
useful for tablets or capsules having pesticide formulations. A
film coating can protect the handler from coming in direct contact
with the active ingredient in the formulations. In addition, a
bittering agent, such as denatonium benzoate or quassin may also be
incorporated in the pesticidal formulations, the coating or both.
The compositions can also be powdered for being pressed tablets or
filled into pre-manufactured gelatin capsules.
[0081] Additionally, the formulations may also be used to supply
nutrients for the beneficial microorganisms used in agriculture or
those present in the rhizosphere area of the growing crops.
Essential nutrients such as cobalt and vanadium may be complexed by
the biosurfactants or the penetrants and made available for these
beneficial microorganisms.
[0082] The penetrants and/or compositions may also be applied on
the soil surface to enhance water permeability and nutrients
availability, as well as to improve soil structure. The penetrant
alone without active agents may also be used for the mentioned
purposes. The compositions may be applied by being injected through
an irrigation system. As such, the penetrants in the invention can
be used to enhance the penetration of water, active agents, or both
into seeds, plant cuttings, trees, and soils. Improved water
penetration using penetrants is beneficial for seed germination and
for nutrient distribution in the soil and plants.
[0083] The penetrants may also be added to pre-formulated
pesticidal preparations that are used as tree treatment agents.
This is especially useful for formulations used in the tree
injection industry (trunk or root flare injections). It can also
assist in increasing the effectiveness of the herbicide in
herbicidal formulations.
[0084] In another embodiment, penetrants can be used in bait
formulations or pheromone traps to enhance the effectiveness of the
active agent and to improve penetration through the pest. This is
particularly beneficial for insecticides, pheromone traps, ant
baits, and in mollusk or snail baits.
[0085] According to another embodiment, formulations used in the
tree injection industry can be applied to enhance the distribution
and translocation of the active agents. This method also reduces
the number of holes drilled in the tree as compared to application
methods of prior art. The new method includes drilling the holes at
right angles or orthogonal to the radii of the tree and parallel to
the soil surface. The holes can be bored inside the water
conducting cambium tissue under the bark. The holes can be drilled
in a tangential position, and the holes can be drilled at angle
positions ranging between 90 degrees (for maximum contact with the
cambium layer) to the radii to 160 degrees angle to the radii. As
such, the injections may be done at about 90 to about 120 degree
angles with respect to the radii of the tree trunk. In any event,
the holes can be bored at any angle that is not congruent or
aligned with the radii or substantially orthogonal to the tangent.
The holes may be bored at a slightly downward position to secure
the injected material in the hole.
[0086] FIG. 2A is a schematic diagram illustrating the prior art
orientation of a therapeutic capsule 18 in a tree 10. As shown, in
the prior art the capsule 18 is inserted into the tree 10 so that
it passes through the bark 12 and into the phloem 14. Usually, the
capsule 18 does not extend into the heartwood 16; however, the
prior art orientation allows it to be possible for the capsule 18
to extend into the heartwood 16. In part, this is because the
orientation of the capsule 18 has been aligned with the radii 22 of
the tree. That is, a hole is bored into the tree 18 so as to be
aligned with the radii 22 and orthogonal to the tangent 24.
Accordingly, a deep enough hole or capsule 18 can be extended into
the heartwood 16.
[0087] FIGS. 2B-2C are schematic diagrams illustrating embodiments
of capsule 18 orientation in accordance with the present invention.
As such, the capsule 18 is inserted into the outer surface 20 of
the tree 10 at an angle .alpha. that is not aligned with the radii
24. Also, the capsule 18 is not at an angle .beta. that is
orthogonal with the tangent 24 because the radii 22 of a tree 10 is
orthogonal to the tangent 24, wherein the sum of .alpha. and .beta.
is equal to 90 degrees. Accordingly, by inserting the capsule 18 at
an angle of .alpha. or .beta., the contents of the capsule 18 can
be delivered into the tree 18 more efficiently, as described
herein.
[0088] For example, the capsule 18 can be oriented at an angle
28a-j that is not aligned with the radii 22 or orthogonal with the
tangent 24. This can include insertion angles 28, such as .alpha.
or .beta., can be as follows: from about 5 to about 10 degrees
(28a); from about 10 to about 15 degrees (28b); from about 15 to
about 15 degrees (28c); from about 20 to about 25 degrees (28d);
from about 20 to about 30 degrees (28e); from about 30 to about 40
degrees (28f); from about 40 to about 50 degrees (28g); from about
50 to about 60 degrees (28h), from about 60 to about 80 degrees
(28i), and from about 70 to about 85 degrees (28j). In another
embodiment, the angles 28a-j can be representative to the downward
angle that the hole and/or capsule 18 is oriented with respect to
the ground, wherein an angle of 0 degrees represents a horizontal
orientation and 90 degrees represents a vertical orientation.
[0089] The new method of injection can ensure that the treating
agent is in direct contact with more conductive tissues or the
phloem for better distribution and faster treatment. This may
prevent the accumulation and loss of active ingredients in the
heartwood area or the nonconductive tissues. In addition, reducing
the number of holes bored in the trees minimizes the potential risk
of infection by decay causing organisms or secondary infestation by
insect borers at the site of injection. This method can be used for
all trees but is particularly important for Dicotyledonous
Angiosperm species. It is also beneficial for certain
monocotylednous types of trees, such as palm, where the conductive
vessels occupy 4 to 5 percent of the total tissues. This method may
be employed with any type of formulations (liquid, solid, or paste)
used in the tree injections industry.
[0090] For instance, liquid injections, gel injections, and solid
capsules can be used in trunk tree injections for improving the
health of the tree. For example, a DMSO-Imidacloprid Gel
formulation can provide enhanced protection against pests when the
composition is administered into the hole drilled into the tree, or
simply applied to the outside of the tree.
[0091] In another embodiment, the action of pesticides can be
enhanced by the use of penetrants. Penetrants enhance the activity
of pesticides and improve their penetration through pests such as
insects, fungi, and bacteria. This can be particularly important
for tree borers, their larva and eggs, or both. An unexpected
result has been achieved when MSM and DMSO were added to
insecticide formulations of cyalothrin or acephate. This
combination greatly improves the effectiveness of the insecticides.
Tests with cyalothrin or acephate with penetrants sprayed on
grasshoppers and caterpillars showed a much higher kill rate and in
a shorter period of time than in the absence of penetrants. The
results of the test are provided in Table 1.
TABLE-US-00001 TABLE 1 EFFECT OF ACEPHATE FORMULATIONS ON
GRASSHOPPER SURVIVAL Acephate Treatments 0% 0.084% 0.084% + MSM
0.084% + DMSO Time (hrs) Grasshopper Survival Rate 4.25 100 100 100
75 5.5 100 100 75 75 6.5 100 100 50 50 7.5 100 75 50 50 9.25 100 75
25 25 14 100 50 0 0 24 100 25 0 0 32 100 0 0 0
[0092] Dry effervescent solid formulations can be prepared using an
organic acid, such as citric acid or malic acid, and a carbonate
salt (e.g., MgCO3, CaCO3) to generate carbon dioxide gas upon
contacting tree sap after being injected into a tree. This may help
in faster translocation of the active ingredient. The injection
site may be sealed to prevent the carbon dioxide gas from escaping.
The concentrations of the individual ingredients in the
formulations can be varied within a relatively wide range.
[0093] Generally, the formulations can be prepared by mixing the
needed amounts of the ingredients with one another in no particular
order. The process may involve heating one or all the components at
a desired temperature. For example, a pre-measured amount of MSM is
melted in a vessel (e.g., a steam jacketted kettle) that is capable
of being stirred. A temperature of about 110.degree. C. is
sufficient to melt the MSM. The bioactive agent (e.g., insecticide
imidacloprid) is then added and dissolved in the molten mixture. If
desired, other additives such as molding adjuvants are then added,
and the mixture is thoroughly blended. Particular forms or moldings
may be formed directly from the molten mixture by the procedures
outlined herein or well-known in the art.
[0094] If a controlled release formulation is desired, a
pre-measured amount of solubility control agent, such as stearic
acid, is added as a molten liquid or as a solid to the
MSM-imidacloprid mix described above. The mix may be extruded,
molded, granulated, or ground into fine granules.
[0095] Another preparation procedure is accomplished by mixing all
the needed ingredients together in a V-Mixer and pressed using a
tablet press. For example a measured amount of polyvinyl
pyrrolidone or MSM is mixed with acephate then pressed using a
tablet press. If necessary, additives such as lubricants may be
used in the formulation.
[0096] The following is a partial list of the active compounds that
may be included in the present formulations and treatments, but
does not include all the compounds that can be used in connection
with the invention. Those of skill in the art, upon learning of the
disclosure made herein, will recognize that the principles of the
invention can be applied using other compounds.
[0097] Example of insecticidal, acaricidal and nematicides active
substances include Abamectin, Acephate, Acriathrin, Alanycarb,
Aldicarb, Aldocycarb, .alpha.-methrin, Amitraz, Aphidan,
Avermectin, Azadiractinn, Azinphos A and M, Azocyclotin, Bacillus
thuringesis,
4-bromo-2-(4-chlorophenyl)-1-(ethoxymethyl)-5-(trifluoro-methyl)-1H-pyrro-
lo-3-carbonitrile, Bendiocarb, Benfuracarb, Bensultap,
.beta.-cyfluthrin, Bifenthrin, Brofenprox, Bromophos, Bufencarb,
Buprofezin, Butocarboxim, Butoxycarboxim, Butylpyridaben,
Cadusafos, Carbaryl, Carbofuran, Carbophenothion, Carbosulphan,
Cartap, Chloethocarb, Chlorethoxyfos, Chlorfenapyr,
Chlorfenvinphos, Chlorfluazuron, Chlormephos, Chlorpyrifos,
cis-Resmethrin, Clocythrin, Clofentezine, Cloprothrin, Cyanophos,
Cyfluthrin, Cyhalothrin, Cyhexatin, Cypermethrin, Cyromazine,
.delta.-methrin, Demeton, Diafenthiuron, Diazinon, Dichlofenthion,
Dichlorvos, Dicliphos, Dicrotophos, Diethion, Diflubenzuron,
Dimefox, Dimethoate, Dimethylvinphos, Dioxathion, Disulfoton,
Edifenphos, Emamectin, Esfenvalerate, Ethiofencarb, Ethion,
Ethofenprox, Ethoprophos, Etrimphos, Fenamiphos, Fenazaquin,
Fenbutatin oxide, Fenitrothion, Fenobucarb, Fenothiocarb,
Fenoxycarb, Fenpropathrin, Fenpyrad, Fenpyroximate, Fenthion,
Fenvalerate, Fipronil, Fluazinam, Fluazuron, Flucycloxuron,
Flucythrinate, Flufenoxuron, Flufenprox, Fluvalinate, Fonophos,
Formothion, Fosthiazate, Fubfenprox, Furathiocarb, Heptenophos,
Hexaflumuron, Hexythiazox, Imidacloprid, Iprobenfos, Isazophos,
Isofenphos, Isoprocarb, Isoxathion, Ivermectin, X-cyhalothrin,
Lufenuron, Malathion, Mecarbam, Mevinphos, Mesulfenphos,
Metaldehyde, Methacrifos, Methamidophos, Methidathion, Methiocarb,
Methomyl, Metolcarb, Mevinphos, Milbemectin, Monocrotophos,
Morphothion, Moxidectin, Naled, Nitenpyram, Oils, Omethoate,
Oxamyl, Oxydemethon-m, Oxydeprofos, Parathion, Permethrin,
Phenthoate, Phorate, Phosalone, Phosmet, Phosphamidon,
Phosphamidon, Phoxim, Pirimicarb, Pirimiphos, Profenophos,
Promecarb, Propaphos, Propoxur, Prothiophos, Prothoate, Pymetrozin,
Pyrachlophos, Pyradaphenthion, Pyresmethrin, Pyrethrum, Pyridaben,
Pyrimidifen, Pyriproxifen, Quinalphos, salts of fatty acids (e.g.,
sodium, potassium, ammonium and the like), Salithion, Sebufos,
Silaflutofen, Spinosad, Sulfotep, Sulprofos, Tebufenozide,
Tebufenpyrad, Tebupirimphos, Teflubenzuron, Tefluthrin, Temephos,
Terbam, Terbufos, Tetrachlorvinphos, Thiafenox, Thiamethoxam,
Thiodicarb, Thiofanox, Thiometon, Thionazin, Tralomethrin,
Triarathen, Triazophos, Triazuron, Trichlorfon, Triflumuron,
Trimethacarb, Vamidothion, Xylylcarb, and Zetamethrin.
[0098] Examples of fungicides active agents include 2-aminobutane,
2-anilino-4-methyl-6-cyclopropyl-pyrimidine,
2',6'-dibromo-2-methyl-4'-trifluoromethoxy-4'-trifluoromethyl-1,3-thiazol-
e-5-carboxanilide,
2,6-dichloroN-(4-trifluoromethylbenzyl)-benzamide,
(E)-2-methoxyimino-N-methyl-2-(2-phenoxyphenyl)-acetamide;
8-hydroxyquinoline sulphate; methyl
(E)-2-{2-[6-(2-cyanophenoxy)-pyrimidin-4-yloxy]-phenyl}-3-methoxyacrylate-
, methyl (E)-methoximino-[alpha-(o-tolyloxy)-o-tolyl]-acetate,
2-phenylphenol (OPP), Aldimorph, Ampropylfos, Anilazine,
Azaconazole, Azoxystrobin, Benalaxyl, Benodanil, Benomyl,
Fenarimol, Triadimefon, Benodanil, Fenpropimorph, Triadimenol,
Kitazin, Fosetyl, Tridemorph, Binapacryl, Biphenyl, Bitertanol,
Blasticidin-S, Boscalid, Bromuconazole, Bupirimate, Buthiobate,
Furalaxyl, Triforine, Carbendazim, Imazalil, Captafol, Captan,
Carbendazim, carbonate salts as potassium carbonate, Carboxin,
Chloroneb, Chloropicrin, Chlorothalonil, Chlozolinate, Copper
compounds, Cufraneb, Cymoxanil, Cyproconazole, Cyprofuram,
Dichlorophen, Diclobutrazol, Dichlofluanid, Diclomezin, Dicloran,
Diethofencarb, Difenoconazole, Dimethirimol, Dimethomorph,
Diniconazole, Dinocap, Diphenylamine, Dipyrithion, Ditalimfos,
Dithianon, Dodine, Drazoxolon, Nuarimol, Oxycarboxin, Dodemorph,
Prochloraz, Edifenphos, Epoxyconazole, Etaconazol, Ethirimol,
Etridiazole, Fenarimol, Fenbuconazole, Fenfuram, Fenitropan,
Fenpiclonil, Fenpropidin, Fenpropimorph, Fentin salts, Ferimzone,
Fluazinam, Fludioxonil, Fluoromide, Fluquinconazole, Flusilazole,
Flusulphamide, Flutolanil, Flutriafol, Folpet, Fosetyl-aluminium,
Fuberidazole, Furalaxyl, Furmecyclox, Guazatine, Hexachlorobenzene,
Hexaconazole, Hprodione, Hsoprothiolane, Hymexazol, imazalil,
imibenconazole, iminoctadine, Iprobenfos, Kasugamycin, Mancopper,
Mancozeb, Maneb, Manganese compounds, Mepanipyrim, Mepronil,
Metalaxyl, Metconazole, Methasulphocarb, Methfuroxam, Metirarn,
Metsulphovax, Myclobutanil, Nickel dimethyldithiocarbamate,
Nitrothal-isopropyl, Nuarimol, Ofurace, natural oils, Oxadixyl,
Oxamocarb, Oxycarboxin, Pefurazoate, Penconazole, Pencycuron,
Phosdiphen, Phthalide Pimaricin, Piperalin, Polyoxin, Polysulphide
salts, Probenazole, Prochloraz, Procymidone, Propamocarb,
Propiconazole, Propineb, Pyrazophos, Pyrifenox, Pyrimethanil,
Pyroquilon, Quinomethionate, Quintozene, salts of fatty acids
(e.g., sodium, potassium, ammonium, and the like), Sulphur
compounds, Tebucanozole, Tecloftalam, Tecnazene, Tetraconazole,
Thiabendazole, Thicyofen, Thiophanate-methyl, Thiram,
Tolclophos-methyl, Tolylfluanid, Triadimefon, Triadimenol,
Triazoxide, Trichlamide, Tricyclazole, Tridemorph, Triflumizole,
Triforin, Triticonazole, Validamycin A, Vinclozolin, Zinc
compounds, Zineb, and Ziram.
[0099] Examples of bactericides include Bronopol, Dichlorophen,
Nitrapyrin, Nickel dimethyldithiocarbamate, Kasugamycin,
Octhilinone, Furancarboxylic acid, Oxytetracycline, Probenazole,
Streptomycin, Tecloftalam, and Copper compounds.
[0100] Examples of herbicides include the following: Anilides, such
as Diflufenican and Propanil; Arylcarboxylic acids, such as
Dichloropicolinic acid, Dicamba and Picloram; Aryloxyalkanoic
acids, such as 2,4-D, 2,4-DB, 2,4-DP, Fluoroxypyr, MCPA, MCPP and
Triclopyr; Aryloxy-phenoxy-alkanoic esters, such as
Diclofop-methyl, Fenoxaprop-ethyl, Fluazifop-butyl,
Haloxyfop-methyl and Quizalofop-ethyl; Azinones, such as
Chloridazon and Norflurazon; Carbamates, such as Chlorpropham,
Desmedipham, Phenmedipham and Propham; Chloroacetanilides, such as
Alachlor, Acetochlor, Butachlor, Metazachlor, Metolachlor,
Pretilachlor and Propachlor; Dinitroanilines, such as Oryzalin,
Pendimethalin and Trifluralin; Diphenyl Ethers, such as
Acifluorfen, Bifenox, Fluoroglycofen, Fomesafen, Halosafen,
Lactofen and Oxyfluorfen; Ureas, such as Chlortoluron, Diuron,
Fluometuron, Isoproturon, Linuron and Methabenzthiazuron;
Hydroxylamines, such as Alloxydim, Clethodim, Cycloxydim,
Sethoxydim and Tralkoxydim; Imidazolinones, such as Imazethapyr,
Imazamethabenz, Imazapyr and Imazaquin; Nitriles, such as
Bromxynil, Dichlobenil and loxynil; Oxyacetamides, such as
Mefenacet; Sulfonylureas, such as Amidosulfuron,
Bensulfuron-methyl, Chlorimuron-ethyl, Chlorsulfuron, Cinosulfuron,
Metsulfuron-methyl, Nicosulfuron, Primisulfeuron,
Pyrazosulfuron-ethyl, Thifensulfuron-methyl, Triasulfuron and
Tribenuron-methyl; Thiolcarbamates, such as Butylate, Cycloate,
Diallate, EPTC, Esprocarb, Molinate, Prosulfocarb, Thiobencarb and
Triallate; Triazines, such as Atrazine, Cyanazine, Simazine,
Simetryne, Terbutryne and Terbutylazin; triazinones, such as
Hexazinone, Metamitron and Metribuzin; and others, such as
Aminotriazole, Beefuresate, Bentazon, Cinmethylin, Clomazone,
Clopyralid, Difenzoquat, Dithiopyr, Ethofumesate, Fluorochloridone,
Gibberellic acid, Glufosinate, Glyphosate, Isoxaben, Pyridate,
Quinchlorac, Quinmerac, Sulphosate, Tridiphane, Dalapon,
Glyphosine, loxynil, Chlorfluorenol, Dichlorprop, Dichlofop,
Mecoprop, Chlormequat, Diquat, Paraquat, Chloroacetic acid,
Fluazifop, Pyridate, Chlorsulfuron, Flurenol, Sulfometuron, and
natural oils.
[0101] Examples of plant nutrients include those that are customary
inorganic or organic fertilizers for providing plants with macro-
and/or micronutrients. The methods of treatment involving the
foregoing penetrants and the complexing agents are applicable to a
broad range of plant nutrients including nitrogen, phosphorus,
sulfur, and the metals boron, calcium, cobalt, copper, iron,
magnesium, manganese, molybdenum, nickel, potassium, and zinc, or a
mixture thereof. A list of representative metal salts includes
acetates, bicarbonates, carbonates, chlorides, hydroxides,
nitrates, oxides, phosphates, and sulfates or a mixture
thereof.
[0102] Examples of plant growth regulators that can be used include
Gibberilic acid, cytokinins, zeatin, auxins, naphthalene acetic
acid, chlorocholine chloride and ethephon.
[0103] Additional active agents that may be used are disinfectants
or sterilizers customarily used in residential areas, hospitals,
storage structures, and the like. A partial list includes
quaternary ammonium compounds (e.g., n-alkyl-dimethylbenzyl
ammonium chloride, n-alkyldimethylethylbenzyl ammonium chloride,
didecyl dimethyl ammonium chloride), bromonitroalkanols,
peroxyacetic acid, glutaraldehyde, or combinations thereof.
[0104] The invention contemplates a broad range of penetrants,
complexing agents, and active agents, as well as a wide range of
ratios for the components. Although the present invention is
described in considerable detail as to certain preferred versions
of preparations and uses, other versions and uses are possible.
Even though the formulations have been described for use to treat
plants, the active agents may be used in other applications. For
example, the use of the penetrants and/or carriers described in
this invention (e.g., biosurfactants) can be used to deliver
essential minerals, nutrients, and vitamins for humans and animals.
Biosurfactant-nutrient complexes can increase the assimilation and
delivery of nutrients for humans and animals. In addition, the
penetrants can be used to deliver drugs commonly used in the
treatment of human diseases such as cancer.
[0105] According to some embodiments of the invention, the
production of fermentation broth or the microbial metabolites
containing the microbial biosurfactant may be used without
extraction or purification. If desired, extraction and purification
of the biosurfactants can be easily achieved using standard
extraction techniques described in the literature.
[0106] Additionally, by mixing the penetrant/carrier with the
active substance(s), a lower dose is required to achieve the same
therapeutic or nutritional value. Therefore, in another embodiment
of the invention, the amount of active substances used in attaining
the maximum nutritional and therapeutic effects is reduced. As
such, this lowers or abolishes some or all the undesirable side
effects associated with higher doses such as liver toxicity in
humans or animals or phytotoxicity in plants.
[0107] Every year many drugs are rejected or taken off the market
owing to their toxicity. The penetrants/carriers disclosed herein
can be used to reformulate many such drugs, thereby reducing their
toxicity by reducing the dose that is needed to achieve the same
therapeutic or nutritional value, which can prevent the use of such
drugs from being discontinued.
[0108] In one embodiment, the biosurfactant, such as the
rhamnolipid, can be used as active agents to control pests,
especially for plants and animals. Studies showed excellent success
in treating the following pests: insects, mites, nematodes, moss,
algae, amoeba, and parasites using rhamnolipids as the active
agent. Also, the addition of an oil, such as a natural oil, to the
biosurfactants greatly amplifies the efficacy of the
biosurfactants. For instance, weed control by rhamnolipids is not
very effective unless you use high amounts of the rhamnolipid,
which can be cost prohibitive. However, formulating an oil with
rhamnolipids makes the biosurfactant more potent, especially
against small weeds and other pests. More particularly, the
combination of a natural oil and a biosurfactant, such as a
rhamnolipid, is effective in controlling insects (e.g., ants and
grasshoppers) and nematodes. Also, the formulations of rhamnolipid
with oils, such as natural oils enhances the efficacy of the
biosurfactant against various fungi.
[0109] In one embodiment, a biosurfactant, such as a rhamnolipid
can be used as a general preservative. Accordingly, the
biosurfactant can be used as a preservative for tree cuttings,
plant cuttings, flower cuttings, food, oils, cosmetics, beauty
products, shampoos, cleaners, soaps, detergents, and plant
nutrients, especially organic based compositions. For example,
rhamnolipid contained within an oil or nutrients formulation can
prevent microbial growth.
[0110] In one embodiment, a biosurfactant, such as a rhamnolipid
can be used to treat and/or prevent various animal diseases.
Examples of diseases that biosurfactants can be used against
include whirling disease on fish caused by amoeba, hoof disease
such as foot rot on cattle/pigs, and others.
EXAMPLES
[0111] The following examples, studies and illustrations should not
be construed as limiting, and are presented for illustration
purposes only.
Example 1
[0112] A 75% acephate solid formulation is prepared with 25 grams
polyethylene glycol (PEG) and 75 grams acephate. Twenty-five grams
mixture of Polyethylene glycol 1450 and 8000 was melted at
75.degree. C. Seventy-five grams acephate was added to the
premelted PEG with stifling for ten minutes. The material was then
poured into molds to yield capsules with 0.75 grams acephate active
ingredient per capsule.
Example 2
[0113] A 75% acephate slow release formulation is prepared with 15
grams MSM, 10 grams stearic acid, and 75 grams acephate.
Example 3
[0114] A 75% acephate solid formulation is prepared by mixing 25
grams MSM and 75 grams acephate. The mixture is pressed using a
tablet press to yield tablets containing 0.75 grams acephate active
ingredient per tablet.
Example 4
[0115] A homogeneous 75% acephate solid formulation is prepared
with 1.5 grams rhamnolipid (or MSM), 1 gram cellulose, and 7.5
grams acephate.
Example 5
[0116] A 97% acephate solid formulation is prepared by mixing 97
grams acephate and 3 grams polyvinyl pyrrolidone. The material is
pressed into tablets. If desired, the prepared tablets are
encapsulated within a gelatin capsules or coated with polyvinyl
alcohol.
Example 6
[0117] A 50% acephate liquid formulation is prepared with 1 gram
rhamnolipid, 5 grams acephate and 4 grams water.
Example 7
[0118] A 25% acephate gel formulation is prepared with 2.5 grams
glycerol, 0.5 grams DMSO, 4 grams polyethylene glycol 4000, 0.5
grams sodium stearate, and 2.5 grams acephate.
Example 8
[0119] A homogeneous 75% acephate formulation is prepared with 10
grams MSM, 5 grams rhamnolipid, 10 grams cellulose, and 75 grams
acephate.
Example 9
[0120] A 25% imidacloprid liquid formulation is prepared with 7.5
grams DMSO and 2.5 grams imidacloprid.
Example 10
[0121] A 15% imidacloprid gel formulation is prepared with 8.3
grams DMSO, 0.2 grams cellulose, and 1.5 grams imidacloprid.
Example 11
[0122] A 20% imidacloprid formulation is prepared with 80 grams MSM
and 20 grams imidacloprid. Solid MSM granules were melted at a
temperature of 120.degree. C. Twenty grams imidacloprid was added
and stirred in the premelted MSM till the imidacloprid totally
dissolved. The melted composition was poured into molds to yield
capsules containing 0.20 grams imidacloprid per capsule.
Example 12
[0123] A homogeneous 25% Imidacloprid solid formulation is prepared
with 3 grams Polyethylene glycol 1450, 1 gram DMSO, 3.5 grams MSM
and 2.5 grams Imidacloprid.
Example 13
[0124] A 25% Imidacloprid solid formulation is prepared with 6.5
grams sorbitol, 1 gram rhamnolipid, and 2.5 grams Imidacloprid.
Example 14
[0125] A 25% Imidacloprid solid formulation is prepared with 6.5
grams MSM, 1 gram rhamnolipid, and 2.5 grams Imidacloprid.
Example 15
[0126] A 20% Imidacloprid formulation is prepared with 3 grams
glycerol, 4 grams polyethylene glycol 4000, 0.5 grams sodium
stearate, and 2 grams imidacloprid.
Example 16
[0127] A 10% Abamectin liquid formulation is prepared with 7.5
grams DMSO, 1.5 grams glycerol and 1 gram Abamectin.
Example 17
[0128] A homogeneous 10% Abamectin solid formulation is prepared
with 3 grams ethylcellulose, 1 gram rhamnolipid, 5 grams MSM, and 1
gram Abamectin.
Example 18
[0129] A 10% rhamnolipid solid formulation is prepared with 9 grams
MSM and 1 gram rhamnolipid
Example 19
[0130] A homogeneous 20% rhamnolipid solid formulation is prepared
with 40 grams starch, 40 grams cellulose, and 80 grams rhamnolipid
(25% strength). The material was dried at 70 degrees Celsius for 24
hours. The dry formulation was pressed using a tablet press to
yield capsules containing 0.2 grams rhamnolipid.
Example 20
[0131] A homogeneous 10% slow release rhamnolipid formulation was
prepared by mixing 50 grams of the mixture of example 19 with
pre-melted 40 grams PEG 8000 and 10 grams myristic acid. The
material was mixed well while maintained at 75 degrees Celsius. The
final formulation is poured into molds.
Example 21
[0132] A 25% Thiamethoxan formulation is prepared with 7.5 grams
MSM and 2.5 grams Thiamethoxan.
Example 22
[0133] A 70% potassium phosphite solid formulation is prepared with
3 grams sorbitol and 7 grams potassium phosphite.
Example 23
[0134] A 70% potassium phosphite solid formulation is prepared with
20 grams starch, 10 grams rhamnolipid and 70 grams potassium
phosphite. The solid formulation is pressed into tablets.
Example 24
[0135] A 70% potassium phosphite solid slow release formulation is
prepared with 10 grams stearic acid, 20 grams MSM, and 70 grams
potassium phosphite.
Example 25
[0136] A 50% potassium phosphite liquid formulation is prepared
using 50 grams potassium phosphite, 5 grams rhamnolipids, and 45
grams water.
Example 26
[0137] A dry mixture of NPK fertilizer with micronutrients is
prepared using urea, ammonium nitrate, ammonium phosphate,
potassium nitrate, calcium and magnesium chloride, and iron,
manganese, zinc, and copper sulfate, and sodium borate. Half of the
final blend was mixed with dry rhamnolipid (example 19) to yield a
homogeneous formulation with the following analysis: 5-5-5 plus
0.2% Ca, 0.2% Mg, 0.1% Mn, 0.1% Fe, 0.1% Zn, 0.02% Cu, and 0.015%
B. The final concentration of the rhamnolipid in the mix was about
12.5%. The other half was mixed with starch instead of rhamnolipid
to yield the same concentration of nutrients in both blends. The
mixtures were used to treat cabbage and tomato plants to determine
yield and leaf tissues elemental analysis.
Example 27
[0138] A mixture of NPK was prepared in liquid formulation.
Gluconate/citric acid buffer was used to maintain the blend at pH
of 4.5-5 units. The final concentrations of the nutrients were
similar to the analysis in the dry fertilizer formulation of
Example 26. The final formulations contained 0 or 10% rhamnolipid
concentration. The liquid mixtures were diluted 100 or 200 times
and used to treat cabbage and tomatoes leaves.
[0139] In all experiments, whether the material was applied to a
soil or leaf, the presence of rhamnolipid and/or biosurfactant in
the nutrient mix was associated with enhanced plant growth and
improved the uptake of most nutrients.
Example 28
[0140] A slow release dry formulation was prepared using the same
ingredients as Example 26. Liquid rhamnolipid broth at 10%
rhamnolipid concentration was intermittently sprayed on the
fertilizer blend and gradually dried at 60.degree. degrees Celsius.
Starch was sprinkled on the mix to prevent the material from
clumping. The final mixture of the blend contained about 2.5%
rhamnolipid concentration as coating.
Example 29
[0141] A homogeneous gel formulation was prepared by mixing 50
grams of rhamnolipid solution (25% strength) and 5 grams DMSO in 50
grams of crosslinked swellable polyacrylamide granules. Rhamnolipid
solution was totally impregnated in the granules in less than 20
minutes. The material was dried in the oven at 70 degrees Celsius.
While the gel may be in certain applications, it is preferable to
be in a dry form. The material may be used to treat pathogens such
as fungi and nematodes. For soil, root flares, and tree injection
applications, it is preferable to impregnate pre-molded
polyacrylamide spikes with the active agent, such as rhamnolipid.
The spikes can be dried to facilitate application and to increase
effectiveness in soil applications.
Example 30
[0142] Citrus leafminer is a serious problem for citrus growers in
Florida, Australia, and the Mediterranean countries. It attacks all
varieties of citrus, but grapefruit, lemon and lime are more
susceptible to infestation than other citrus varieties. Leafminers
have a short developmental time and as many as 6-13 generations per
year can be expected depending on foliage flushing cycles, nitrogen
fertility, humidity, and temperature. The hatched larvae of citrus
leafminer form serpentine mines in leaves and occasionally in the
citrus fruit. Pupation occurs in folds on the edges of leaves.
Leafminer larva is characterized by a central line of frass and is
protected within the leaf. Infestation levels of up to 20 miners
per leaf are common. Like borers, leafminer is not easily
controlled by insecticidal spray.
[0143] Treatments were started at the beginning of the first
foliage flush. Using formulations of Examples 1, 3, and 10, ten and
twenty year old citrus (lemons, grapefruit, oranges) trees were
treated, which were susceptible to natural infestation with the
citrus miner. Each treatment consisted of four trees. Each of the
two-year old seedlings was treated with two tablets inserted in the
soil. Thirty leaves were collected from each treatment and the
mines were counted. Qualitative measurement of the severity of
infestation was observed. Each of the older trees was treated with
three tablets inserted in the trunk at equal spacing. The trees
were observed during two new growth flushes over two months period,
and the results are set forth in Table 2.
TABLE-US-00002 TABLE 2 EFFECT OF ACEPHATE AND IMIDACLOPRID
FORMULATIONS ON INFESTATION CITRUS TREES WITH CITRUS LEAFMINER.
Treatments Time (days Control Example 1 Example 3 Example 10 after
treatment) Average leaf damage area (%) 30 63 27 6 18 60 72 36 21
12
[0144] As seed in Table 2, the acephate formulation of Example 3,
with the penetrant MSM, was the fastest and most effective
treatment. Almost all infestation symptoms were eliminated in the
presence of MSM. Imidacloprid formulation (Example 10) with MSM was
also effective and had a longer residual activity. It was also
observed that the treated trees with the formulation of Example 1
had inconsistent control on some branches. Some branches were more
infested than the other branches on the four treated trees. While
the physical processes that yielded these results are not critical
to the understanding or use of the invention, it is believed that
the presence of the penetrant has either improved the translocation
of the pesticides throughout the trees or enhanced its penetration
through the larvae and inaccessible leaf tissues or both.
Example 31
[0145] Aspen trees heavily infested with flat-head borers were
treated using acephate (Examples 1, 2) and imidacloprid (Example
10) tablets. Each treatment consisted of six trees (about 7-8 inch
trunk diameter) that were injected with three tablets per tree. The
studies started at the first sign of borers infestation. Total
borer activities and frass accumulation under the trees stopped
within one month of the initiation of the studies. Both
insecticidal treatments with MSM had the same effect. Acephate
treatment without the penetrant MSM (Example 1) had less than 60
percent effectiveness as compared to the treatments with a
penetrant. Control trees (no insecticide) were infested with borers
for the whole season.
Example 32
[0146] Two Aspen trees infected with leaf spot fungal disease were
each treated with four tablets containing phosphite (Example 23).
All the new leaves exhibited a healthy growth and were free of
fungal infection for the rest of the season.
Example 33
[0147] Into each 1-liter water bottle containing 0 or 500 ppm DMSO,
a tablet containing 0.2 grams rhamnolipid (Example 19) was added.
Ten-mosquitoes larvae were transferred into each of the bottles.
Additional bottle contained ten-mosquitoes larvae in 1-liter water
was used as control. Total death of the larva was observed in about
2 hours and 40 minutes in the bottle containing rhamnolipid alone.
The presence of DMSO with the rhamnolipid caused death in less than
2 hours. No death was observed in the control treatment.
Example 34
[0148] A naturally infested ants mound was treated with four
tablets of example 5. The mound was free of ants for more than two
months after the treatment.
[0149] The processes, methods of use and examples of components
listed in the invention are illustrative and not inclusive. The
invention may be embodied in other specific forms without departing
from its spirit or essential characteristics. The described
embodiments are to be considered in all respects only as
illustrative and not restrictive. The appended claims are presented
to illustrate the embodiments of the invention disclosed
herein.
* * * * *