U.S. patent application number 16/593693 was filed with the patent office on 2021-04-08 for insect repelling composition.
The applicant listed for this patent is GLOBAL BIOLIFE INC.. Invention is credited to Daryl L. THOMPSON, Scott M. TRUESDELL.
Application Number | 20210100243 16/593693 |
Document ID | / |
Family ID | 1000005476172 |
Filed Date | 2021-04-08 |
United States Patent
Application |
20210100243 |
Kind Code |
A1 |
THOMPSON; Daryl L. ; et
al. |
April 8, 2021 |
INSECT REPELLING COMPOSITION
Abstract
A composition and method for insect repellent is provided. The
composition in one form has on a weight percentage basis 10-20%
2,6-dimethyl-7-octen-2-ol; 0.1-5% 2,6-octadienal, 3,7-dimethyl-;
1-10% benzyl benzoate; 0.01-2% citral; 1-10% hexamethylindanopyran;
10-40% lavender oil; 20-50% Lemon Oil Argentina; 5-15% Lime Oil
Distilled Mexican; 0.01-3% limonene; 5-15% rosemary oil; and
optionally 0.1-10% an insect repellent active ingredient selected
from the group consisting of N,N-Diethyl-meta-toluamide (DEET),
ethyl butylacetylaminopropionate and picaridin. The composition has
insect repellent properties.
Inventors: |
THOMPSON; Daryl L.; (Winter
Haven, FL) ; TRUESDELL; Scott M.; (Bethesda,
MD) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
GLOBAL BIOLIFE INC. |
Bethesda |
MD |
US |
|
|
Family ID: |
1000005476172 |
Appl. No.: |
16/593693 |
Filed: |
October 4, 2019 |
Current U.S.
Class: |
1/1 |
Current CPC
Class: |
A01N 25/02 20130101;
A01N 37/18 20130101; A01N 65/22 20130101; A01N 31/04 20130101; A01N
65/36 20130101; A01N 43/40 20130101; A01N 35/02 20130101; A01N
37/10 20130101 |
International
Class: |
A01N 37/18 20060101
A01N037/18; A01N 65/22 20060101 A01N065/22; A01N 25/02 20060101
A01N025/02; A01N 43/40 20060101 A01N043/40; A01N 65/36 20060101
A01N065/36; A01N 35/02 20060101 A01N035/02; A01N 37/10 20060101
A01N037/10 |
Claims
1. A composition comprising, on a weight percent basis: 10-20%
2,6-dimethyl-7-octen-2-ol; 0.1-5% 2,6-octadienal, 3,7-dimethyl-;
1-10% benzyl benzoate; 0.01-2% citral; 1-10% hexamethylindanopyran;
10-40% lavender oil; 20-50% Lemon Oil Argentina; 5-15% Lime Oil
Distilled Mexican; 0.01-3% limonene; and 5-15% rosemary oil.
2. The composition of claim 1, further comprising 0.1-10% an insect
repellent active ingredient selected from the group consisting of
N,N-Diethyl-meta-toluamide (DEET), ethyl butylacetylaminopropionate
and picaridin.
3. The composition of claim 1, further comprising on a weight basis
0.1-10% alcohol selected from the group consisting of isopropyl,
ethyl, and methyl.
4. The composition of claim 1, comprises: 12-18%
2,6-dimethyl-7-octen-2-ol; 0.1-1% 2,6-octadienal, 3,7-dimethyl-;
2-5%--benzyl benzoate; 0.01-1% citral; 2-5%--hexamethylindanopyran;
25-30% lavender oil; 30-40% Lemon Oil Argentina; 5-10% Lime Oil
Distilled Mexican; 0.01-0.1% limonene; and 5-10% rosemary oil.
5. The composition of claim 4, further comprising 1-10% an insect
repellent active ingredient selected from the group consisting of
N,N-Diethyl-meta-toluamide (DEET), ethyl butylacetylaminopropionate
and picaridin.
6. The composition of claim 4, further comprising on a weight basis
0.1-1% alcohol selected from the group consisting of isopropanol,
ethanol and methanol.
7. The composition of claim 1 further comprises an inactive
carrier, which in combination thereby forms a topical location.
8. The composition of claim 1, wherein the composition is
formulated as a solution for application as a spray or mist.
9. A method for repelling insects comprising deploying a
composition comprising, on a weight percent basis: 10-20%
2,6-dimethyl-7-octen-2-ol; 0.1-5% 2,6-octadienal, 3,7-dimethyl-;
1-10% benzyl benzoate; 0.01-2% citral; 1-10% hexamethylindanopyran;
10-40% lavender oil; 20-50% Lemon Oil Argentina; 5-15% Lime Oil
Distilled Mexican; 0.01-3% limonene; and 5-15% rosemary oil.
10. The method of claim 9, wherein the composition further
comprises 0.1-10% an insect repellent active ingredient selected
from the group consisting of N,N-Diethyl-meta-toluamide (DEET),
ethyl butylacetylaminopropionate and picaridin.
11. The method of claim 9, wherein deploying the composition
comprises applying the composition to an individual to thereby
repel insects from the individual.
12. The method of claim 9, wherein deploying the composition
comprises spraying the composition in an area where one wishes to
repel insects.
13. The method of claim 9, wherein deploying the composition
comprises placing the composition in an area where one wishes to
repel insects.
14. The method of claim 9, wherein deploying the composition
comprises burning the composition to thereby release its
constituents into the surrounding environment to thereby repel
insects in the surrounding environment.
15. The method of claim 9, wherein deploying the composition
comprises spraying or misting the composition formulated as a
solution for application as a liquid.
16. The method of claim 9, wherein the composition comprises:
12-18% 2,6-dimethyl-7-octen-2-ol; 0.1-1% 2,6-octadienal,
3,7-dimethyl-; 2-5%--benzyl benzoate; 0.01-1% citral;
2-5%--hexamethylindanopyran; 25-30% lavender oil; 30-40% Lemon Oil
Argentina; 5-10% Lime Oil Distilled Mexican; 0.01-0.1% limonene;
and 5-10% rosemary oil.
17. The method of claim 16, wherein the composition further
comprises 0.1-10% an insect repellent active ingredient selected
from the group consisting of N,N-Diethyl-meta-toluamide (DEET),
ethyl butylacetylaminopropionate and picaridin.
18. The composition of claim 5, further comprising on a weight
basis 0.1-10% alcohol selected from the group consisting of
isopropyl, methanol and ethanol.
19. The composition of claim 2, further comprises an inactive
carrier, which in combination thereby forms a topical location.
20. The composition of claim 2, wherein the composition is
formulated as a solution for application as a spray or mist.
21. The method of claim 10, wherein deploying the composition
comprises applying the composition to an individual to thereby
repel insects from the individual.
22. The method of claim 10, wherein deploying the composition
comprises spraying the composition in an area where one wishes to
repel insects.
23. The method of claim 10, wherein deploying the composition
comprises placing the composition in an area where one wishes to
repel insects.
Description
FIELD OF THE INVENTION
[0001] The present invention relates to a composition for repelling
insects and in particular a composition comprising various
constituents in a formulation that has insect repelling
properties.
BACKGROUND OF THE INVENTION
[0002] Insects provide valuable functions including but not limited
to pollination of plants, being a food source and other positive
roles. However, some insects have undesirable effects which include
but are not limited to carrying and transferring diseases as well
as being nuisances, e.g., insects that bite. For example, ticks and
mosquitos carry diseases that affect animals and humans.
[0003] Mosquitoes are responsible for most human illnesses with an
average 500 million cases resulting in three million deaths
annually. Ninety percent of these cases occur in Africa alone with
2.5 billion at risk globally. Women are particularly at risk due to
the increased attractiveness to predatory mosquitoes due to the
increased alkalinity of their skin.
[0004] Further, mosquito borne diseases are one of the most deadly
threats to the human population. The strategies for the prevention
of mosquito vectored dieses must be discovered as risk of these
diseases will incrementally increase as natural occurrence of
mosquito habitat spreads due to global warming. Presently there is
a global population of approximately 10 million species of insects.
Of those it has been determined that 10,000 of those actively feed
on blood and the amount of those that feed on humans would number
around 100. The insects that prey on humans are required to deploy
an array of sensitive chemoreceptor networks that work in specific
coordination to locate prey.
[0005] Currently today the best strategies that exist for mosquito
protection for humans is N,N-Diethyl-meta-toluamide (DEET), ethyl
butylacetylaminopropionate (trade name IR3535) and picaridin.
Although these chemicals are effective, they lack serious
limitations that the following invention seeks to solve. DEET,
ethyl butylacetylaminopropionate, and picaridin are effective in
that they stimulate a key receptor of the mosquito's chemosensory
array to illicit a repellent response. This primary receptor is
called the Or47a and Or83b DEET-like receptor. Affecting this
receptor by use of DEET, ethyl butylacetylaminopropionate, or
picaridin proves to be its own limitation in which it which it only
affects this receptor. This strategy only serves to create single
method in which to repel mosquitoes or predatory insects. The
mosquito can still relay on other chemosensory receptors to locate
prey which makes the DEET receptor ineffective.
[0006] It has been universally recognized that the use of botanical
extracts to repel mosquitoes have met with limitations due to the
toxic effects of some of the chemicals that they contain at certain
levels. The toxic effects of most mosquito repelling fragrances or
oils have limited effectiveness due to the other toxic chemicals
present in them. The following is a list of examples of popular
mosquito repelling fragrances/oils and their toxic effects; anise
(Pimpinella anisum) carcinogenic due to methyl eugenol, basil
(Ocimum sp) carcinogenic due to methyl eugenol, bergamot (Citrus
bergamia) phototoxic skin irritant due to d-limonene, cajeput
(Melaleuca alternifolia) phototoxic skin irritant due to methyl
eugenol, citronella (Cymbopogon nardus) skin irritant due to methyl
eugenol and citral, citrus oil (Citrus sp) phototoxic skin irritant
due to bergapten and d-limonene, clove (Syzygium aromaticum) skin
irritant due to methyl eugenol, lemon bush (Lippia javanica) skin
irritant due to citral, geranium (Pelargonium graveolens) skin
irritant due to citral, ginger (Zinziber sp) skin irritant due to
citral, huon (Langarostrobus franklini) skin irritant due to methyl
eugenol, lemongrass (Cympogon cintratus) skin irritant due to
citral, lime (Citrus aurantifolia) phototoxic skin irritant due to
d-limonene, litsea (Litsea cubebia) skin irritant due to citral,
marigold (Tagates minuta) phototoxic, wormseed (Chenopodium
ambrosiodes) liver toxicity, mint (Mentha piperata) skin irritant
due to trans-2-hexanol, nutmeg (Myristica fragrans) skin irritant
due to methyl eugenol, palmarosa (Cymbopogon martini) carcinogenic
due to methyl farnesol, pennyroyal (Menthyl pulegium) toxic, pine
(Pinus sylvestris) phototoxic, rosemary (Rosemarinus officinalis)
skin irritant due to methyl eugenol, rue (Ruta chalepensis)
phototoxic due to psoralene, thyme (Thymus vulgaris) skin irritant
due to trans-2-hexanol, violet (viola odorata) skin irritant due to
trans-2-hexanol.
[0007] Fragrant oils such as citronella, rosemary, and eucalyptus
have been used for to repel insects for thousands of years. These
fragrant oils are comprised on VOC (volatile organic compounds)
produced by flowers and fruit. These oils are collected as extracts
from their respective sources and are technically described as an
accord. An accord is a suite of chemicals that are grouped together
to create a specific odor. These accords may be duplicated to by
perfumers to create specific fragrances and are comprised of a top,
middle and base note. The volatility of these components are
highest with the top note, somewhat volatile with the middle note
and least volatile with the base note.
[0008] In the case of citronella, an oil found in many botanical
sources and known for its repellent activity was determined to be
comprised of several mixtures of oils. It was discovered that the
accord that makes up the fragrance is comprised of sub-oils that
have repellent factors and other sub oils that are not
repellent.
[0009] For instance citronella is of 18-20% geraniol, limonene
9-11%, methylisoeugenol 7-11%, citronellol 6-8%, and citronellal
5-15%. It is interesting to point out that only the geraniol,
limonene, and citronella oils have mosquito repellent properties
while the remaining oils in the accord are for other purposes such
as defense or attractants.
[0010] This is also the same for eucalyptus oil that is comprised
of 60-80% cineole oil with the remaining 40-20% being trace oils.
The remaining trace oils are alpha-pinene 9%, beta-pinene 1.5%,
alpha phellandrene 1.5%, delta limonene 12%, 1,8 cineole 70%,
camphor 0.1%, and sabinene, 0.3%.
[0011] Research conducted shows that fragrant accords in most
insect (e.g., mosquito) repelling oils are only partially
responsible for repelling insects with the remainder of the
fragrant oils utilized as an attractant for pollinating insects or
acting to signal health characteristics such as defense pheromones
to nearby plants of similar species.
[0012] For instance, the fragrant aroma of the common tomato plant
is an excellent example. The leaves' cellular structures are
comprised of glandular trichomes that contain crystals and oils in
their bulbous sections. These structures contain oils that are
responsible for several biological functions including plant
defense. The tomato leaf chemical constituents are tomatine,
(Z)-3-hexenal, (E)-2-hexenal, eugenol, 1,8 cineole, caryophyllene,
b-phellandrene, humulene, linalool. Each chemical of the tomato has
either a specific function or synergistic function. As with the
case of the fragrance of tomato, through research it was determined
that tomatine is an anti-membrane defense chemical that is used to
prevent biofilm formation of attacking snails, bacteria, or fungi.
(Z)-hexenal is involved with wound healing as it possesses
anti-microbial capability by inhibiting JA signaling of invading
bacteria and fungi. (E)-2-hexenal, although similar to
(Z)-3-hexenal, acts as an attractant for beneficial predatory
insects. The chemical b-phellandrene is a chemical attractant known
for luring caterpillar predatory mites to the site of injury. This
leaves the chemicals eugenol, 1,8 cineole, caryophyllene, humulene,
and linalool as the sole chemicals of the tomato fragrant accord
responsible for repelling insects.
[0013] Another key drawback with the use of natural botanical
extracts of plants with known mosquito repelling properties is that
is that some of the chemical constituents that make up the accord
are actual chemical attractants for mosquitoes. This can be clearly
seen in the chemical accord of the well-known mosquito repelling
extract, cedar oil that contain cedrol, isolongifolene, and
dehydroneolingifolene. It is well recognized that the replication
cycle of mosquito borne disease is one of the largest biological
threats to mankind. All of the viruses that affect man share a
unique but similar cycle. A good example would be the malaria
infection cycle. The cycle begins with a malaria infected mosquito
biting and infecting a human host. The malaria parasite then grows
and waits in the human host for the next mosquito to bite the host.
The parasite then travels from the host to the mosquito where it
now becomes infected as well. The cycle repeats with the malaria
parasite traveling between the two human and mosquito hosts. It is
important discuss that the malaria parasite has evolved to emit a
chemical signal that "messages" the mosquito to come and pick up
the parasite. While nearing maturity inside the human host, the
parasite will begin to emit chemical signatures that attract the
mosquitoes to the infected human host.
SUMMARY OF THE INVENTION
[0014] The present invention relates to various compositions which
are formulations comprising several constituents. The constituents,
together, as well as when combined with existing conventional,
existing repellents such as (DEET), picaridin, ethyl
butylacetylaminopropionate (trade name IR3535) and other known
mosquito repellents, provide compositions that have enhanced
synergistic effects in terms of insect repelling properties as
compared with the components separately. Existing mosquito
repellents target only gustatory receptors in insects. The present
formulation uses a multiple receptor approach by targeting
ionotropic, gustatory, and olfactory receptors in insects to
provide a synergistic action to repel insects as well as inhibit
the ability of insects to detect and seek prey.
[0015] Some of the constituents are found in botanical plants.
Further, some of the components or constituents are fragrances
produced by plants and such plants may have a multitude of other
chemicals that have properties which may or may not have insect
repellent characteristics. These include chemo-sensory signaling
for defense, attractants, wound healing, etc. An improved mosquito
repellent may be potentiated by formulation of a repellent that
only incorporates the insect repellent active chemicals from a vast
array of mosquito repellent fragrances. Such a formulation would be
superior in that it would contain key chemical chemosensory
inhibitors to inhibit the Or47a and Or83b DEET receptor, the AgOr65
protein receptor, the cpA carbon dioxide receptor, and the AeegOr4
or AaegOr103 sulcatone human specific receptor. The formulation may
be realized by critical analysis and extrapolation of these
specific chemoreceptor specific compounds of all botanical
fragrances that are known to have mosquito or insect repellent
properties.
[0016] In addition to superior insect repellent properties,
formulations of the present composition are safe for humans and
animals.
[0017] Some formulations of the present invention are directed to a
more useful strategy would be a complex formulation that can
inhibit all of the mosquitoes' chemosensory package. This would
include the AgOr65 protein receptor, the cpA carbon dioxide
receptor and the AaegOr4 or Aaeg103 receptor that senses sulcatone
which is uniquely emitted by human hosts.
[0018] The present invention, in one form, relates to a
composition, on a weight percentage basis as follows: [0019] 10-20%
2,6-dimethyl-7-octen-2-ol; [0020] 0.1-5% 2,6-octadienal,
3,7-dimethyl-; [0021] 1-10% benzyl benzoate; [0022] 0.01-2% citral;
[0023] 1-10% hexamethylindanopyran; [0024] 10-40% lavender oil;
[0025] 20-50% Lemon Oil Argentina; [0026] 5-15% Lime Oil Distilled
Mexican; [0027] 0.01-3% limonene; and [0028] 5-15% rosemary
oil.
[0029] Optionally, the composition can comprise 0.1-10% alcohol
such as ethanol, isopropanol and methanol.
[0030] The present invention, in another form, relates to a
composition, on a weight percentage basis as follows: [0031] 10-20%
2,6-dimethyl-7-octen-2-ol; [0032] 0.1-5% 2,6-octadienal,
3,7-dimethyl-; [0033] 1-10% benzyl benzoate; [0034] 0.01-2% citral;
[0035] 1-10% hexamethylindanopyran; [0036] 10-40% lavender oil;
[0037] 20-50% Lemon Oil Argentina; [0038] 5-15% Lime Oil Distilled
Mexican; [0039] 0.01-3% limonene; [0040] 5-15% rosemary oil; and
[0041] 0.1-10% an insect repellent active ingredient selected from
the group consisting of N,N-Diethyl-meta-toluamide (DEET), ethyl
butylacetylaminopropionate and picaridin. [0042] Optionally, the
composition can comprise 0.1-10% alcohol such as ethanol,
isopropanol and methanol.
[0043] The present invention, in another form, relates to a
composition, on a weight percentage basis as follows: 12-18%
2,6-dimethyl-7-octen-2-ol; [0044] 0.1-1% 2,6-octadienal,
3,7-dimethyl-; [0045] 2-5%--benzyl benzoate; [0046] 0.01-1% citral;
[0047] 2-5%--hexamethylindanopyran; [0048] 25-30% lavender oil;
[0049] 30-40% Lemon Oil Argentina; [0050] 5-10% Lime Oil Distilled
Mexican; [0051] 0.01-0.1% limonene; [0052] 5-10% rosemary oil, and
[0053] Optionally 0.1-10% an insect repellent active ingredient
selected from the group consisting of N,N-Diethyl-meta-toluamide
(DEET), ethyl butylacetylaminopropionate and picaridin.
[0054] Optionally, the composition can comprise 0.1-10% alcohol
such as ethanol, isopropanol and methanol.
[0055] The present invention, in another form thereof, relates to a
method for repelling insects using a composition, on a weight
percentage basis as follows: [0056] 10-20%
2,6-dimethyl-7-octen-2-ol; [0057] 0.1-5% 2,6-octadienal,
3,7-dimethyl-; [0058] 1-10% benzyl benzoate; [0059] 0.01-2% citral;
[0060] 1-10% hexamethylindanopyran; [0061] 10-40% lavender oil;
[0062] 20-50% Lemon Oil Argentina; [0063] 5-15% Lime Oil Distilled
Mexican; [0064] 0.01-3% limonene; [0065] 5-15% rosemary oil; and
[0066] Optionally 0.1-10% an insect repellent active ingredient
selected from the group consisting of N,N-Diethyl-meta-toluamide
(DEET), ethyl butylacetylaminopropionate and picaridin. [0067]
Optionally, the composition can comprise 0.1-10% alcohol such as
ethanol, isopropanol and methanol.
[0068] In still another form thereof, a method for repelling
insects includes deploying a composition comprising, on a weight
percent basis as follows: [0069] 12-18% 2,6-dimethyl-7-octen-2-ol;
[0070] 0.1-1% 2,6-octadienal, 3,7-dimethyl-; [0071] 2-5%--benzyl
benzoate; [0072] 0.01-1% citral; [0073]
2-5%--hexamethylindanopyran; [0074] 25-30% lavender oil; [0075]
30-40% Lemon Oil Argentina; [0076] 5-10% Lime Oil Distilled
Mexican; [0077] 0.01-0.1% limonene; [0078] 5-10% rosemary oil, and
[0079] Optionally 0.1-10% an insect repellent active ingredient
selected from the group consisting of N,N-Diethyl-meta-toluamide
(DEET), ethyl butylacetylaminopropionate and picaridin. [0080]
Further, optionally, the composition can comprise 0.1-10% alcohol
such as ethanol, isopropanol and methanol.
[0081] The composition can be formulated as a solid, a liquid such
as an oil or a lotion, etc. The composition can be deployed by
topically applying the composition to an individual (human or
animal), spraying the composition on the individual or in an
environment in which one wishes to repel insects, burning the
composition, etc.
[0082] Advantages of the present composition and method include but
are not limited to a more effective insect including mosquito
repellent than conventional compositions.
DETAILED DESCRIPTION
[0083] The present composition functions as a repellent of insects
including mosquitoes. The mechanism by which the present invention
operates varies depending on the specific constituents in the
composition. The composition includes constituents such as
fragrances that act on an insect's olfactory sensory neurons. Other
constituents in the present composition affect an insect's other
senses.
[0084] In one preferable formulation, the present composition
achieves a superior insect repellent that focuses on repellent
factors while avoiding limitations of toxicity to humans, animals
or other living things including plants to which one wishes to
repel insects.
[0085] Referring specifically to how various formulations of the
present composition affect insects and in particular mosquitoes,
each mosquito olfactory sensory neuron expresses one odorant
receptor which recognizes specific structural features or epitopes
in odorant molecules. Axons of neurons expressing the same receptor
converge onto a single glomerus. Therefore a given odorant may have
structural features that are recognized by odorant receptors Or83b,
Or47a, Or4, Or103, and cpA that activate the corresponding
glomeruli. Another odorant may have different epitopes and may
activate alternate receptors. A third type of odorants may have
completely different epitopes and activate several receptors
simultaneously. Therefore, an odorant receptor and its
corresponding glomerulus can be activated by several different
odorants, but each odorant is likely to elicit a unique pattern of
glomeruli activation. This pattern constitutes an odorant specific
neural pattern that the mosquito utilizes to find prey.
[0086] One aspect of the present composition focuses on specific
components or constituents that inhibit these olfactory receptors
either specifically or universally to effectively "blind" the
insect (e.g., mosquito) to human prey. This strategy allows one to
select specific constituents and respective concentrations for
inclusion in formulations of the present composition sufficient to
produce an insect repellent that has synergistic, superior insect
repellent properties as compared with that of DEET, IR3535, or
picaridin alone which only affect singular receptors.
[0087] In accordance with another aspect of the present
composition, the composition can be formulated to make an
individual to which the composition is applied "blind" to insects
such as but not limited to mosquitos or other biting insects, by
inhibiting the protein receptors that detect body odors in humans
or animals. These specialized receptors detect specific proteins of
body odors emitted by humans. These odors are sulcatone and lactic
acid. The mosquito antennae have specialized receptors (AaegOr4,
AaegOr65, and AaegOr103) that detect human body odors sulcatone and
lactic acid that are specific in locating human prey. All of these
receptors require the function of P450 isozymes for the receptors
to detect these human specific odorants. It would be a unique
strategy to incorporate key chemicals into a repellent that
sufficiently inhibits the function of the AaegOr4, AaegOr65, and
AaegOr103 receptors. Successful deactivation of these key receptors
via P450 isozyme inhibition would blind the mosquito to the
presence of a human host. Accordingly, several formulations of the
present composition include constituents for the purpose of
blinding mosquito sulcatone and lactic acid receptors by
inactivation of native receptor P450 isozymes.
EXAMPLES
[0088] The following are examples of formulations and uses of the
present composition.
Example 1
[0089] Formula 1--The composition of Formula 1 has, on a weight
percentage basis the following:
TABLE-US-00001 1. 2,6-dimethyl-7-octen-2-ol 14.20% 2.
2,6-octadienal, 3,7-dimethyl- 0.44% 3. ethyl alcohol 0.15% 4.
benzyl benzoate 3.55% 5. citral 0.06% 6. hexamethylindanopyran
3.55% 7. lavender oil 28.80% 8. Lemon Oil Argentina 35.00% 9. Lime
Oil Distilled Mexican 7.10% 10. limonene 0.06% 11. rosemary oil
7.10%
Experiments
[0090] Table 1 (below) demonstrates insect repellency of Formula 1
to inhibit both landing and probing (feeding behavior) of
mosquitoes.
TABLE-US-00002 TABLE 1 `Neat` pure Formula 1 - 100% concentration
Time Landings Probes 1 hour after application 100% repellency 100%
repellency 2 hours after application 100% repellency 100%
repellency
[0091] Collagen membranes were used as a skin analog for testing
the liquid test substances. The collagen membranes were moistened
with water and the surface was dried prior to the applications to
provide a texture and consistency that was similar to human skin.
The applications were conducted with the collagen membranes by
shaking the test substances well, then applying the test substance
onto the membranes until wet and then gently rubbing the test
substance into the membranes.
[0092] The membranes were placed on top of water moistened paper
towels (lightly moistened) to maintain a "skin like" consistency by
preventing complete moisture loss from the membranes while aging.
The membranes were placed on the paper towels with the untreated
side in contact with the paper towels and water was added to the
paper towels as needed to maintain moisture during the aging
process. Each test substance was evaluated at 1 and 2 hours after
the applications. Each evaluation consisted of two (2) replicates
per age.
[0093] Twenty-five (25) female mosquitoes were released inside a
1'.times.1' cage and the mosquitoes were held without food for at
least 2 hours prior to testing. The cage had a 1'.times.1' wooden
cover on the top of the cage with an approximate 2.5''.times.6''
removable section in its center. The section was removable to
provide an opening in the top of the cage for the test surface and
for the mosquitoes to try to feed on the test subject's arm above
the test surface. Mesh was placed on the top side of the test
surface to prevent direct contact of the test surface with the test
subject's arm and disposable wood spacers were placed on top of the
top cover to elevate the test subject's arm from the test substance
and to prevent the mosquitoes from being able to feed on the test
subject.
[0094] An untreated pre-treatment evaluation was conducted prior to
testing the treated test surface by counting the number of
mosquitoes that landed and probed on an untreated test surface
during a 5-minute time period. The treated surface was evaluated in
the same manner as the untreated surface and the repellency was
calculated by comparing the number of landing and probes during the
pre-treatment evaluation to the number of landing and probes during
the treatment evaluation. The study was conducted using two
different test subjects for each test substance and aged
evaluation.
TABLE-US-00003 TABLE 2 As active ingredient of Formula 1 in a
lotion* % Active ingredient Time Landings Probes 0.25% 6 hours
after 83% repellency 95% repellency application 0.25% 8 hours after
42% repellency 50% repellency application 1% 6 hours after 63%
repellency 83% repellency application 1% 8 hours after 73%
repellency 78% repellency application 5% 6 hours after 78%
repellency 91% repellency application 5% 8 hours after 75%
repellency 83% repellency application (*The lotion formulation
consists of 0.25%, 1% and 5% Formula 1 and the following inactive
ingredients by weight: 81-85.8% water 5.6% cetearyl alcohol 2.4%
ceteareth-20 2% isopropyl myristate 2% soybean oil 0.995% glycerin
0.900% phenoxy ethanol 0.10% ethylhexylglycerin
[0095] Collagen membranes were used as a skin analog for testing
the liquid test substances. The collagen membranes were moistened
with water and the surface was dried prior to the applications to
provide a texture and consistency that was similar to human skin.
The applications were conducted to the collagen membranes by
shaking the test substances well, then applying the test substance
onto the membranes using a 1 gram/600 cm2 application rate and then
gently rubbing the test substance into the membranes.
[0096] The membranes selected for the untreated controls were
moistened with water but did not receive any other application. The
membranes were placed on top of water moistened paper towels
(lightly moistened) to maintain a "skin like" consistency by
preventing complete moisture loss from the membranes while aging.
The membranes were placed on the paper towels with the untreated
side in contact with the paper towels and water was added to the
paper towels as needed to maintain moisture during the aging
process. Test substances were evaluated at 6 and 8 hours after the
applications. Each evaluation consisted of 4 replicates for the
controls and 4 replicates for each test substance per age.
[0097] Twenty-five (25) female mosquitoes were released inside a
1'.times.1' cage and the mosquitoes were held without food for at
least 2 hours prior to testing. The cage had a 1'.times.1' wooden
cover on the top of the cage with an approximate 2.5''.times.6''
removable section in its center. The section was removable to
provide an opening in the top of the cage for the test surface and
for the mosquitoes to try to feed on the test subject's arm above
the test surface. Mesh was placed on the top side of the test
surface to prevent direct contact of the test surface with the test
subject's arm and disposable wood spacers were placed on top of the
top cover to elevate the test subject's arm from the test substance
and to prevent the mosquitoes from being able to feed on the test
subject. An untreated pre-treatment evaluation was conducted prior
to testing the treated test surface by counting the number of
mosquitoes that landed and probed on an untreated test surface
during a 5-minute time period. The treated surface was evaluated in
the same manner as the untreated surface and the repellency was
calculated by comparing the number of landing and probes during the
pre-treatment evaluation to the number of landing and probes during
the treatment evaluation. The study was conducted using two
different test subjects for each test substance and aged
evaluation.
[0098] It will now be clear that the present composition in its
various formulations provides features and advantages not found in
prior insect repellents. The present composition can be formulated
to have strong insect repellent properties while being safe for
humans and animals.
[0099] Further, the composition can be formulated to have superior
mosquito repelling properties based on its constituents including
fragrances which are created by selection of active extracts that
effect multiple repellent strategies of predator insects such as,
but not limited to, mosquitos, lice, ticks, fleas, flies, bed bugs
and mites.
[0100] Further, the present composition can be optimized by
selecting the specific constituents in desired amounts to achieve a
desired insect repellent property based on the desired insect to
repel and based on a selected desire to protect mammals including
humans and animals from insects including biting insects.
[0101] Selection of desirable constituents for inclusion of
formulations of the presented composition are based on inhibition
of key insect receptors which include mosquito receptors for
repelling mosquitos. This may be accomplished synergistically by
inhibition of carbon dioxide receptors, body odor receptors,
DEET-like receptors or Dopamine Receptors. Progressive inhibition
of synaptic firing of potentials in these key receptors lead result
in the insect finding the human target undesirable and causes
aversion to feeding.
[0102] Further, the composition can be modified such that when
applied to humans, the human is "invisible" or unappealing to
insects such as mosquitos by specially selecting particular
isolates comprising the fragrance linked to ultra-stimulate key
receptors utilized by mosquitos or other insects to select
prey.
[0103] In various forms of the present composition, the
constituents work synergistically to effect known DEET receptors of
an insect such as a mosquito. For example there are two specific
DEET receptors Or83B and Or47a. The contemplated formula contains
linalool that is known to affect these specific receptors
respectively.
[0104] In addition, the present composition can be formulated to
inhibit key chemical signatures that modulate mosquito feeding
behavior. Doing so would result in reducing or controlling the
infection rate of malaria carried by mosquitos. It is known that
the malaria parasite will cause infected individuals to "outgas"
chemical attractants that attract mosquitoes (pinene and limonene).
It is the object of the invention to utilize a-pinene or limonene
or both as chemical "blinding agents" by over stimulating mosquito
sensory receptors that detect these chemicals. Over stimulation of
these key receptors will elicit an avoidance behavior of
predatorial mosquitoes.
[0105] In addition, the composition can be formulated with specific
chemical constituents that render an insect "blind" for sensing
carbon dioxide discharge from animals and human hosts. The
receptors in particular are the gr1, gr2, and gr3 "gustatory"
receptors containing the cpA receptor sensory cluster. It would be
contemplated that the formulations would contain ethyl pyruvate,
7-a-beta-nepatalactone, methyl salicylate either independently or
in combination as gustatory inhibitors.
[0106] The composition can also be formulated to contain specific
chemical isolates that "blind" insect receptors AaegOr4, AaegOr65,
and AaegOr103 by deactivation or inhibition of P450 isozymes found
in the receptor. Deactivation of protein specific receptors would
blind the mosquito to the presence of sulcatone and lactic acid
odors produced by human targets. These contemplated isolates are
myrcene, borneol, and pinene that actively deactivate the sulcatone
and lactic acid specific protein receptors of the mosquito by
direct and passive inhibition of the receptors native neuronal P450
isozymes.
[0107] Alternatively, the present composition can be formulated to
prevent malaria infection by creating a topical formulation of
botanical abstracts that are toxic to malaria (P. falciparum)
sporozoites. It is contemplated that certain chemical components of
botanical extracts are toxic to malarial sporozoites and
plasmodium. It is further contemplated that direct reduction of
malaria infection may be accomplished as the mosquito proboscis
comes into contact with these botanical extracts at the initiation
of penetration of the host.
[0108] In yet another alternative, the present composition can be
formulated to contain chemicals that inhibit mosquitoes from
developing learned behavior to avoid the aversion causing
properties of DEET. It has been proven that mosquitoes can learn
behavior that bypasses and reduces the effectiveness of DEET. This
learned behavior has been well identified as one of the key factors
that reduce the effectiveness of DEET. It is the object of the
invention that the mosquito repelling formula contain monoterpenes
as a means of inhibiting loss of DEET effectiveness by tolerance
learning. This would include limonene.
[0109] Further, modifying the constituents in the present
composition will have an effect to alter the overcall fragrant
signature of the resulting composition which through routine
experimentation and optimization will result in an insect repellent
to perform as a repellent of a desired insect or for a particular
application or use.
* * * * *