U.S. patent application number 13/359017 was filed with the patent office on 2012-05-17 for topical compositions comprising inorganic particulates and an alkoxylated diphenylacrylate compound.
Invention is credited to Mirela Cristina Ionita-Manzatu, Linda Josephine Najdek, Milanka Susak, Ismail Ahmed Syed.
Application Number | 20120121673 13/359017 |
Document ID | / |
Family ID | 43050790 |
Filed Date | 2012-05-17 |
United States Patent
Application |
20120121673 |
Kind Code |
A1 |
Susak; Milanka ; et
al. |
May 17, 2012 |
Topical Compositions Comprising Inorganic Particulates And An
Alkoxylated Diphenylacrylate Compound
Abstract
A topical composition of improved spreadability and aesthetical
appeal is provided, which contains inorganic particulates in
combination with an alkoxylated diphenylacrylate compound.
Preferably, the topical composition is a sunscreen composition that
contains inorganic or physical sunscreen agents in combination with
an alkoxylated .alpha.-cyanodiphenylacrylate compound, which is
characterized by improved photo-protection of the skin and is
effective in preventing/reducing photo-damage of the skin upon
exposure to sunlight or other sources of light in the ultraviolet
(UV), visible, and infrared (IR) ranges.
Inventors: |
Susak; Milanka; (North York,
CA) ; Syed; Ismail Ahmed; (Ronkonkoma, NY) ;
Najdek; Linda Josephine; (East Islip, NY) ;
Ionita-Manzatu; Mirela Cristina; (Old Bethpage, NY) |
Family ID: |
43050790 |
Appl. No.: |
13/359017 |
Filed: |
January 26, 2012 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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12771237 |
Apr 30, 2010 |
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13359017 |
|
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61175261 |
May 4, 2009 |
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Current U.S.
Class: |
424/401 ;
424/60 |
Current CPC
Class: |
A61K 33/24 20130101;
A61K 9/5026 20130101; A61K 2300/00 20130101; A61K 8/27 20130101;
A61K 33/24 20130101; A61K 33/30 20130101; A61Q 17/04 20130101; A61P
17/00 20180101; A61K 2300/00 20130101; A61K 33/30 20130101; A61K
47/32 20130101; A61K 31/12 20130101; A61K 47/06 20130101; A61K
47/24 20130101; A61K 2300/00 20130101; A61K 31/12 20130101; A61K
33/30 20130101; A61K 2300/00 20130101; A61K 2300/00 20130101; A61K
9/0014 20130101; A61K 33/24 20130101; A61K 47/10 20130101; A61K
31/12 20130101; A61K 8/40 20130101; A61K 2300/00 20130101; A61K
8/29 20130101 |
Class at
Publication: |
424/401 ;
424/60 |
International
Class: |
A61K 8/40 20060101
A61K008/40; A61Q 17/04 20060101 A61Q017/04; A61K 8/02 20060101
A61K008/02 |
Claims
1. A topical composition comprising at least one inorganic
particulate material and an alkoxylated diphenylacrylate compound
in a pharmaceutically or cosmetically acceptable carrier.
2. The topical composition of claim 1, wherein the at least one
inorganic particulate material comprises at least one metal
oxide.
3. The topical composition of claim 1, wherein the at least one
inorganic particulate material comprises a physical sunscreen agent
selected from the group consisting of titanium dioxide particles,
zinc oxide particles, and mixtures thereof.
4. The topical composition of claim 1, wherein the alkoxylated
diphenylacrylate compound is an alkoxylated
.alpha.-cyanodiphenylacrylate having the formula (I): ##STR00004##
wherein one or both of R.sub.1 and R.sub.2 is a straight or
branched-chain C.sub.1-C.sub.30 alkoxy radical, any non-alkoxy
radical R.sub.1 or R.sub.2 is hydrogen, and R.sub.3 is a straight
or branched-chain C.sub.1-C.sub.30 alkyl radical.
5. The topical composition of claim 4, wherein one or both of
R.sub.1 and R.sub.2 is a straight or branched-chain C.sub.1-C.sub.8
alkoxy radical.
6. The composition of claim 1, wherein the alkoxylated
diphenylacrylate compound is an alkoxylated
.alpha.-cyanodiphenylacrylate having the formula (III), (IV) or
(V): ##STR00005## wherein R.sub.3 is a straight or branched-chain
C.sub.1-C.sub.30 alkyl radical.
7. The topical composition of claim 1, wherein the alkoxylated
diphenylacrylate compound is .alpha.-ethylhexyl
.alpha.-cyano-.beta.-(4-methoxyphenyl)-.beta.-phenylacrylate.
8. The topical composition of claim 1, wherein the at least one
inorganic particulate material is entrapped by collapsed polymeric
shells to form microspheres having an average particle size ranging
from about 1 micron to about 50 microns.
9. The topical composition of claim 1, further comprising one or
more organic or chemical sunscreen agents selected from the group
consisting of 4,4'-t-butyl methoxydibenzoylmethane,
2-ethylhexylsalicylate, 3,3,5-trimethylcyclohexylsalicylate,
2-ethylhexyl p-methoxycinnamate, 2-hydroxy-4-methoxybenzophenone,
2,2-dihydroxy-4-methoxybenzophenone,
2,4-bis-{4-(2-ethyl-hexyloxy)-2-hydroxyl-phenyl}-6-(4-methoxyphenyl)-1,3,-
5-triazine, methylene bis-benzotriazolyl tetramethylbutylphenol,
terephthalylidene dicamphor sulfonic acid, diethylhexyl
2,6-naphthalate, digalloyltrioleate, ethyl
4-[bis(hydroxypropyl]aminobenzoate, glycerol p-aminobenzoate,
methylanthranilate, p-dimethylaminobenzoic acid or aminobenzoate,
2-ethylhexyl p-dimethylaminobenzoate,
2-phenylbenzimidazole-5-sulfonic acid,
2-(p-dimethylaminophenyl)-5-sulfoniobenzoxazoic acid, and mixtures
or combinations thereof.
10. The topical composition of claim 1, further comprising at least
one DNA repair enzyme.
11. The topical composition of claim 1, further comprising glycerin
or a C.sub.2-C.sub.4 alkylene glycol.
12. The topical composition of claim 1, further comprising methyl
trimethicone.
13. A topical composition having an SPF ranging from about 15 to
100 comprising .alpha.-ethylhexyl
.alpha.-cyano-.beta.-(4-methoxyphenyl)-.beta.-phenylacrylate, an
inorganic particulate selected from the group consisting of zinc
oxide, titanium dioxide, and mixtures thereof.
14. The topical composition of claim 13, wherein the inorganic
particulate is entrapped by collapsed polymeric shells to form
microspheres having an average particle size ranging from about 1
micron to about 50 microns.
15. The topical composition of claim 13, further comprising at
least one nonvolatile silicone having a viscosity ranging from
about 5 to 250,000 centistokes at 25.degree. C.
16. The topical composition of claim 13, further comprising at
least one silicone elastomer.
17. The topical composition of claim 13, further comprising
trimethylsiloxysilicate.
18. The topical composition of claim 13, further comprising at
least one volatile paraffinic hydrocarbon selected from the group
consisting of isododecane, isohexadecane, and mixtures thereof.
Description
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a divisional of U.S. Ser. No.
12/771,237, filed Apr. 30, 2010, which claims priority from U.S.
Provisional Patent Application No. 61/175,261 filed May 4,
2009.
FIELD OF THE INVENTION
[0002] The invention relates to topical compositions with skin care
or cosmetic properties. Specifically, the invention relates to
topical compositions containing inorganic particulates in
combination with an alkoxylated diphenylacrylate compound, which
functions to improve dispersion (i.e., reduced coagulation) of the
inorganic particulates and thereby achieve better
feel/spreadability of such compositions on the skin. More
specifically, when the inorganic particulates are physical
sunscreen particles, such as titanium dioxide and/or zinc oxide
particles, the topical compositions of the present invention are
characterized by enhanced photo-protection and are particularly
useful for preventing/reducing photo-damage of the skin upon
exposure to sunlight or other sources of light in the ultraviolet
(UV), visible, and infrared (IR) ranges.
SUMMARY OF THE INVENTION
[0003] The present invention provides a topical composition
comprising at least one inorganic particulate material and a
diphenylacrylate, more specifically an alkoxylated diphenylacrylate
compound, in a pharmaceutically or cosmetically acceptable carrier.
It has been discovered that the alkoxylated diphenylacrylate
compound, which is a lipophilic organic compound, surprisingly and
unexpectedly improves dispersion of the inorganic particulate
material in the pharmaceutically or cosmetically acceptable carrier
and reduces potential agglomeration.
[0004] In a preferred, but not necessary, embodiment, the present
invention provides a topical sunscreen composition for protecting
the skin against photo-damage upon exposure to UV radiation, which
comprises at least one physical sunscreen agent selected from the
group consisting of titanium dioxide and zinc oxide and an
alkoxylated .alpha.-cyanodiphenylacrylate compound in a
pharmaceutically or cosmetically acceptable carrier. The
alkoxylated .alpha.-cyanodiphenylacrylate compound preferably has
the formula (I):
##STR00001##
wherein one or both of R.sub.1 and R.sub.2 is a straight or
branched-chain C.sub.1-C.sub.30 alkoxy radical, any non-alkoxy
radical R.sub.1 or R.sub.2 is hydrogen, and R.sub.3 is a straight
or branched-chain C.sub.1-C.sub.30 alkyl radical. It has been
discovered that such an alkoxylated .alpha.-cyanodiphenylacrylate
compound, when combined with a physical sunscreen agent,
surprisingly and unexpectedly enhances the photo-protective effect
of the physical sunscreen agent, even in absence of any chemical
sunscreen agent. Therefore, in a most preferred embodiment, the
topical sunscreen composition of the present invention is
substantially free of chemical sunscreen agents, such as, for
example, dibenzoylmethane compounds or derivatives thereof.
DETAILED DESCRIPTION OF THE INVENTION, AND THE PREFERRED
EMBODIMENTS THEREOF
[0005] The term "percentage" or "%" as used herein in connection
with the amount or concentration of an ingredient or component in a
composition refers to the percentage by total weight of the final
composition, unless otherwise specified.
[0006] The term "substantially free of" or "in absence of" as used
herein refers to an amount that is equal to or less than 1% by
total weight of the final composition.
[0007] The inventors of the present invention discovered that
.alpha.-cyanodiphenylacrylate compounds are effective in
facilitating the dispersion of inorganic particulates and improving
the overall aesthetical appeal of the resulting topical composition
(e.g., feel and spreadability on skin). This discovery is
particularly surprising and unexpected in light of the fact that
the inorganic particulates, such as metal oxides, are highly
charged particles, while the .alpha.-cyanodiphenylacrylate
compounds are lipophilic organic compounds.
[0008] Furthermore, the inventors discovered that when the
inorganic particulates are physical sunscreen agents, such as
titanium dioxide and/or zinc oxide particles, the combination
thereof with the .alpha.-cyanodiphenylacrylate compound
surprisingly and unexpectedly enhances the efficacy of the overall
composition in protecting the skin against UV-induced damages, even
in absence of any chemical sunscreen agents, such as butyl
methoxydibenzoylmethane (hereinafter "Avobenzone") and/or octyl
methoxycinnamate (hereinafter "OMC").
[0009] Any inorganic particulate material suitable for topical
application can be used in the present invention, which include,
but are not limited to titanium dioxide, zinc oxide, iron oxides,
mica, titanated mica, alumina, talc, pearl powder, calcium
carbonate, calcium phosphate, calcium silicate, calcium sulfate
(gypsum), magnesium carbonate, magnesium oxide, magnesium silicate,
magnesium aluminum silicate, magnesium trisilicate, aluminum
silicate, aluminum magnesium silicate, silica, fumed silica,
hydrated silica, spherical silica, silica silylate, bismuth
oxychloride, chalk, kaolin, diatomaceous earth, fuller's earth,
kaolin, sericite, muscovite, phlogopite, lepidolite, biotite,
vermiculite, smectite clays, strontium silicate, metal tungstate,
magnesium, silica alumina, zeolite, tin oxide, barium sulfate,
fluorine apatite, hydroxyapatite, ceramic powder, colloidal
silicone dioxide, boron nitride, hectorite, montmorillonite,
bentonite, attapulgite, titanium hydroxide, trimagnesium phosphate,
and the like.
[0010] Preferred inorganic particulate materials are selected from
metal oxides, such as titanium dioxide, zinc oxide, iron oxides,
magnesium oxide, alumina (or aluminum oxide), tin oxide, and the
like. More preferably, the topical composition of the present
invention is a sunscreen composition that comprises at least one
inorganic sunscreen agent, such as titanium dioxide and zinc oxide,
and most preferably, it comprises a blend of titanium dioxide and
zinc oxide.
[0011] The average particle size of the inorganic particulate
materials is preferably less than 1 micron, more preferably ranging
from about 0.001 micron to about 0.9 micron, and most preferably
from about 0.1 to about 0.5 micron. The inorganic particulate
materials of the present invention can be of any regular or
irregular shape, such as, for example, spherical, cubic,
cylindrical, planar, fibrous, and the like. Such inorganic
particulate materials may either be naked (i.e., uncoated) or be
surface-treated or coated with one or more layers of coating
materials to impart desirable surface properties thereto. For
example, the inorganic particulate materials may be coated with a
hydrophilic or hydrophobic polymer, or encapsulated/entrapped in a
hydrophilic or hydrophobic polymeric matrix, to improve the
compatibility of such inorganic particulate materials with the
carrier medium.
[0012] In a preferred, but not necessary embodiment of the present
invention, the inorganic particulate materials are entrapped in a
collapsed polymeric shell to form microspheres having an average
particle size ranging from about 1 micron to about 50 microns. The
collapsed polymeric shell can be formed of any synthetic or natural
crosslinked or un-crosslinked polymer. If the polymer is
crosslinked, it is preferred that it is weakly crosslinked.
Preferably, but not necessarily, the collapsed polymeric shell
comprises at least one synthetic polymer obtained by polymerization
of one or more ethylenically unsaturated monomers to form
homopolymers or copolymers of ethylenically unsaturated monomers or
copolymers of ethylenically unsaturated monomers and one or more
organic groups. Examples of ethylenically unsaturated monomers that
may be suitable include, for example, vinylidene chloride, vinyl
chloride, acrylonitrile, acrylic acid and its corresponding C1-C20
aliphatic or aromatic esters, methacrylic acid and its
corresponding C1-C20 aliphatic or aromatic esters, acrylamide,
methacrylamide, vinyl pyrrolidone, alkenes such as styrene,
ethylene, propylene, butylene, methylpentene, 1,3-butadiene, and
the like. The polymeric shells of the hollow microspheres may also
be formed of suitable synthetic polymers, such as polyesters,
polyamides, polyphthalamides, polyimides, polycarbonates,
polyketones, cellulose acetate, polysulfones, polyphenylene
sulfides, polyphenylene oxides, polylactic acids,
polyvinylpyrrolidone, polystyrene, polyacrylonitrile,
polyacrylamide, polymethylmethacrylate, polyacrylates, and
copolymers of the above-listed polymers. In a particularly
preferred embodiment, the collapsed polymeric shell is formed of a
copolymer of vinylidene chloride, acrylonitrile, and/or methyl
methyacrylate.
[0013] Entrapment of the inorganic particulate materials into the
above-described collapsed polymeric shell can be achieved by first
providing hollow microspheres with deformable polymeric shells
having encapsulated therein an expandable fluid, which are then
mixed with, either sequentially in any order or simultaneously, a
polar organic solvent capable of swelling but not dissolving the
polymeric shells of the hollow microspheres and the inorganic
particulate materials to be entrapped. A gelled mixture is thereby
formed, which contains microspheres with polymeric shells in a
gelled state, which are sufficiently swelled so as to have
micro-channels or through-holes formed therein to allow entry of
the inorganic particulate materials into the microspheres. Such
micro-channels or through-holes in the swelled polymeric shells of
the microspheres also allow exit of the expandable fluid from the
microspheres, thereby causing immediate collapse or implosion of
the polymeric shells and entrapping the inorganic particulate
materials inside the microspheres. Subsequently, the expandable
fluid and the polar organic solvent are removed from the gelled
mixture. Preferably but not necessarily, a film-forming material is
coated over the collapsed polymeric shells to form a
liquid-impermeable membrane thereon, which functions to isolate the
collapsed polymeric shells of the microspheres from any solvent in
the surrounding environment that may swell or otherwise affect the
structural integrity of such polymeric shells. In this manner, the
inorganic particulate materials can be securely entrapped inside
the microspheres with little or no risk of leaking out. The hollow
microspheres as initially provided (i.e., before mixing with the
solid particles and the polar organic solvent) are preferably
expandable hollow polymeric microspheres, each of which contains a
deformable polymeric shell that is gas-tight and has enclosed or
encapsulated therein an expandable fluid. Upon heating, the
enclosed or encapsulated fluid can expand volumetrically to apply
pressure on the interior wall of the deformable polymeric shell. At
the same time, the elevated temperature may cause the polymeric
shell to soften, thereby allowing the entire microsphere to expand
in a manner similar to a balloon. For more details regarding the
structure and composition of the hollow microspheres and the
inorganic particulate entrapment process, see U.S. Patent
Application Publication No. 2009/0155371, the content of which is
incorporated herein by reference in its entirety for all
purposes.
[0014] The inorganic particulate material can be present in the
topical composition of the present invention in an amount ranging
from about 0.1% to about 90%, preferably from about 5% to about
50%, and more preferably from about 10% to about 30%, by total
weight of the composition.
[0015] Although all alkoxylated .alpha.-cyanodiphenylacrylate
compounds are suitable for the practice of the present invention,
preferred alkoxylated .alpha.-cyanodiphenylacrylate compounds for
use in the present invention are those with an alkoxyl substitution
group at the para position of at least one of the phenyl rings,
i.e., those represented by formula (II):
##STR00002##
wherein one or both of R.sub.1 and R.sub.2 is a straight or
branched-chain C.sub.1-C.sub.30 alkoxy radical, more preferably a
straight or branched-chain C.sub.1-C.sub.8 alkoxy radical, any
non-alkoxy radical R.sub.1 or R.sub.2 is hydrogen, and R.sub.3 is a
straight or branched-chain C.sub.1-C.sub.30 alkyl radical. Among
straight or branched-chain C.sub.1-C.sub.8 alkoxy radicals,
preferred are methoxy, ethoxy, n-propoxy, iospropoxy, n-butyoxy,
isobutyoxy, and tert-butoxy radicals. Among straight or
branched-chain C.sub.1-C.sub.30 alkyl radicals, preferred are
methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl,
n-amyl, isoamyl, neopentyl, n-hexyl, n-heptyl, n-octyl,
2-ethylhexyl, decyl and lauryl radicals.
[0016] More preferred species of alkoxylated
.alpha.-cyanodiphenylacrylate compounds include those having the
formulas (III)-(V):
##STR00003##
wherein R.sub.3 is as previously defined.
[0017] Most preferred species of alkoxylated
.alpha.-cyanodiphenylacrylate compound for the practice of the
present invention is .alpha.-ethylhexyl
.alpha.-cyano-.beta.-(4-methoxyphenyl)-.beta.-phenylacrylate
(hereinafter "methoxycrylene"), which is commercially available
from HallStar Company (Chicago, Ill.). Methoxycrylene has been used
in the past for stabilizing certain organic or chemical sunscreen
agents that are susceptible to photo-decomposition upon exposure to
UV radiation, such as Avobenzone and OMC. For more details about
Methoxycrylene, see U.S. Patent Application Publication Nos.
US2009/039322A, US2009/039323A and US2009/042312A, and
International Patent Application Publication No. WO09/020,675A,
which are hereby incorporated by reference in their entireties for
all purposes.
[0018] It has been discovered by the inventors that methoxycrylene
is a surprisingly and unexpectedly effective dispersing agent, and
it can be combined with inorganic particulate materials to form
cosmetic or sunscreen compositions of excellent spreadability with
little or no coagulation.
[0019] Further, it has been discovered by the inventors that
methoxycrylene, when combined with physical sunscreen agents, such
as TiO.sub.2 or ZnO, can synergistically enhance the
photo-protective effect of such physical sunscreen agents, in the
absence of any organic or chemical sunscreens. Nothing in the state
of art teaches, suggests or even contemplates such a synergistic
effect of methoxycrylene in combination with a purely physical
sunscreen system, which is both surprising and unexpected. In
addition, the refractive index (RI) of methoxycrylene is
significantly higher than that of its non-alkoxylated structural
analogs. For example, methoxycrylene has a RI of about 1.59, while
octocrylene, which is a non-alkoxylated structural analog of
methoxycrylene, has a RI of only about 1.56-1.57. The higher RI
value of methoxycrylene allows it to form more transparent (and
therefore more aesthetically acceptable) sunscreen formulations
when combined with titanium dioxide or zinc oxide, which has a RI
value of above 2.
[0020] The alkoxylated diphenylacrylate compound can be present in
the topical composition of the present invention in an amount
ranging from about 0.01% to about 50%, preferably from about 0.1%
to about 20%, and more preferably from about 1% to about 15%, by
total weight of the composition.
[0021] Although not necessarily, the inorganic particulate material
and the alkoxylated diphenylacrylate compound can be formulated
with one or more optional organic or chemical sunscreen agents,
thereby providing sunscreen compositions of high SPF values (e.g.,
SPF measurements of greater than 25, 30, 35, 40, 45, or even 50 or
more). If present, such organic or chemical sunscreen agents may
each range from about 0.01 to 45% by weight of the total
composition.
[0022] Exemplary organic or chemical sunscreen agents that can be
used in combination with the inorganic particulate material and the
alkoxylated diphenylacrylate compound of the present invention
include, but are not limited to UVA and UVB sunscreens, such as
benzophenones and derivatives thereof (e.g., benzophenone-3,
dioxybenzone, sulisobenzone, octabenzone, hydroxy- and/or
methoxy-substituted benzophenones, and benzophenonesulfonic acids
and salts thereof); salicylic acid derivatives (e.g., ethylene
glycol salicylate, triethanolamine salicylate, octyl salicylate,
homomethyl salicylate, and phenyl salicylate); urocanic acid and
derivatives thereof (e.g., ethyl urocanate); p-aminobenzoic acid
(PABA) and derivatives thereof (e.g., ethyl/isobutyl/glyceryl
esters thereof and 2-ethylhexyl p-dimethylaminobenzoate, which is
also referred to as octyldimethyl PABA); anthranilates and
derivatives thereof (e.g., o-amino-benzoates and various esters of
amino-benzoic acid); benzalmalonate derivatives; benzimidazole
derivatives; imidazolines; bis-benzazolyl derivatives;
dibenzoylmethanes and derivatives thereof;
benzoazole/benzodiazole/benzotriazoles and derivatives thereof
(e.g., 2-(2-hydroxy-5-methylphenyl)benzotriazole and methylene
bis-benzotriazolyl tetramethylbutylphenol, which is commonly
referred to as "Tinosorb M"); diesters or polyesters containing
diphenylmethylene or 9H-fluorene substitutional groups;
2-phenyl-benzimidazole-5-sulphonic acid (PBSA);
4,4-diarylbutadienes; cinnamates and derivatives thereof (e.g.,
2-ethylhexyl-p-methoxycinnamate, octyl-p-methoxycinnamate,
umbelliferone, methylumbelliferone, methylaceto-umbelliferone,
esculetin, methylesculetin, and daphnetin); camphors and
derivatives thereof (e.g., 3-benzylidenecamphor,
4-methylbenzylidenecamphor, polyacrylamidomethyl
benzylidenecamphor, benzylidene camphor sulfonic acid, and
terephthalylidene dicamphor sulfonic acid, which is commonly
referred to as "Encamsule"); triazines and derivatives thereof
(e.g.,
2,4-bis-{[4-(2-ethyl-hexyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1,3-
,5-triazine, which is commonly referred to as "Tinosorb S");
naphthalates and derivatives thereof (e.g.,
diethylhexyl-2,6-naphthalate); naphtholsulfonates and derivatives
thereof (e.g., sodium salts of 2-naphthol-3,6-disulfonic and
2-naphthol-6,8-disulfonic acids); dibenzalacetone and
benzalacetonephenone; diphenylbutadienes and derivatives thereof;
di-hydroxynaphthoic acid and salts thereof; o- and
p-hydroxybiphenyldisulfonates; coumarin derivatives (e.g.,
7-hydroxy, 7-methyl, and 3-phenyl derivatives thereof);
azoles/diazoles/triazoles and derivatives thereof (e.g.,
2-acetyl-3-bromoindazole, phenyl benzoxazole, methyl naphthoxazole,
and various aryl benzotriazoles); quinine and derivatives thereof
(e.g., bisulfate, sulfate, chloride, oleate, and tannate salts
thereof); quinoline and derivatives thereof (e.g.,
2-phenylquinoline and 8-hydroxyquinoline salts); tannic acid and
derivatives thereof (e.g., hexaethylether derivatives thereof);
hydroquinone and derivatives thereof; uric acid and derivatives
thereof; vilouric acid and derivatives thereof, and mixtures or
combinations thereof. Salts and otherwise neutralized forms of
certain acidic sunscreens from the list hereinabove are also useful
herein. These organic or chemical sunscreen agents may be used
alone or in combination of two or more. In addition, other known
animal or vegetable extracts having UV light-absorbing ability may
properly be used alone or in combination.
[0023] Organic or chemical sunscreen agents that are particularly
useful for the practice of the present invention are: 4,4'-t-butyl
methoxydibenzoylmethane, 2-ethylhexylsalicylate,
3,3,5-trimethylcyclohexylsalicylate, 2-ethylhexyl
p-methoxycinnamate, 2-hydroxy-4-methoxybenzophenone,
2,2-dihydroxy-4-methoxybenzophenone,
2,4-bis-{4-(2-ethyl-hexyloxy)-2-hydroxyl-phenyl}-6-(4-methoxyphenyl)-1,3,-
5-triazine, methylene bis-benzotriazolyl tetramethylbutylphenol,
terephthalylidene dicamphor sulfonic acid, diethylhexyl
2,6-naphthalate, digalloyltrioleate, ethyl
4-[bis(hydroxypropyl)]aminobenzoate, glycerol p-aminobenzoate,
methylanthranilate, p-dimethylaminobenzoic acid or aminobenzoate,
2-ethylhexyl p-dimethylaminobenzoate,
2-phenylbenzimidazole-5-sulfonic acid,
2-(p-dimethylaminophenyl)-5-sulfoniobenzoxazoic acid, and mixtures
or combinations thereof.
[0024] Although organic or chemical sunscreens can be used in the
topical composition of the present invention, it is not necessary
to include them since the combination of inorganic sunscreen
particles (e.g., TiO.sub.2 and/or ZnO) with the alkoxylated
diphenylacrylate compound provides a sufficient photo-protective
barrier for blocking the harmful UV-A and UV-B radiation.
Preferably, the topical composition of the present invention is
substantially free of any organic or chemical sunscreens, and more
preferably free of dibenzoylmethane derivatives, such as
Avobenzone.
[0025] The inorganic particulate materials and the alkoxylated
diphenylacrylate compound of the present invention can be added
directly to any pharmaceutically or cosmetically acceptable carrier
to form a cosmetic or topical composition. For purpose of the
present invention, pharmaceutically or cosmetically acceptable
carriers are substances that are biologically compatible with human
skin and can be used to formulate active ingredients described
hereinabove and/or hereinafter into a cream, gel, emulsion, liquid,
suspension, powder, nail coating, skin oil, or lotion that can be
topically applied. In the case where the cosmetically acceptable
carrier is in the form of an emulsion, it may contain from about
0.1 to 99%, preferably from about 0.5 to 95%, more preferably from
about 1 to 80% by weight of the total composition of water and from
about 0.1 to 99%, preferably from about 0.1 to 80%, more preferably
from about 0.5 to 75% by weight of the total composition of oil. In
case where the composition is anhydrous it may comprise from about
0.1 to 90 wt % of oil and from about 0.1 to 75 wt % of other
ingredients such as pigments, powders, non-aqueous solvents (such
as mono-, di-, or polyhydric alcohols, etc. In case where the
composition is in the form of an aqueous based gel, solution, or
suspension, it may comprise from about 0.1 to 99 wt % of water and
from about 0.1 to 75 wt % of other ingredients such as botanicals,
non-aqueous solvents, etc.
[0026] Suitable components of the pharmaceutically or cosmetically
acceptable carrier include, but are not limited to: moisturizing
agents, astringent agents, chelating agents, sequestrants,
emulsifiers/surfactants, emollients, preservatives, stabilizers,
abrasives, adsorbents, thickeners, gellants,
solidifying/structuring agents, anti-caking agents, anti-foaming
agents, pH buffering/adjusting agents, binders, film formers,
humectants, pigments, opacifiers, essential oils, fragrances, and
aromatic compounds. The pharmaceutically or cosmetically acceptable
carrier or carriers can be present in the topical or cosmetic
composition of the present invention at an amount ranging from
about 1% to about 99.9%, preferably from about 50% to about 99.5%,
more preferably from about 70% to about 99%, and most preferably
from about 80% to 90% by total weight of the topical or cosmetic
composition.
[0027] The topical or cosmetic composition may contain one or more
skin care additives, which are agents that provide benefits to the
skin, rather than merely improving the physical or aesthetic
characteristics of the topical composition. If present, such skin
care actives may range from about 0.01 to 50%, preferably from
about 0.05 to 35% by weight of the total composition. Exemplary
skin care additives that can be used in the topical or cosmetic
compositions of the present invention include, but are not limited
to: self-tanning agents (e.g. dihydroxyacetone), anti-aging agents,
DNA-repair enzymes, anti-wrinkle agents, anti-acne agents (e.g.,
resorcinol, salicylic acid, and the like), enzyme-inhibiting
agents, collagen-stimulating agents, agents for the eradication of
age spots and keratoses, analgesics, anesthetics, antimicrobials
(e.g., antibacterials, antiyeast agents, antifungal agents, and
antiviral agents), antidandruff agents, antidermatitis agents,
antipruritic agents, antiemetics, anti-inflammatory agents,
antihyperkeratolytic agents, antiperspirants, antipsoriatic agents,
antiseborrheic agents, antihistamine agents, skin lightening
agents, depigmenting agents, skin soothing/healing agents (e.g.,
aloe vera extract, allantoin, and the like), corticosteroids,
hormones, antioxidants, proteins or peptides, vitamins and
derivatives thereof (e.g., vitamin A, vitamin E, vitamin B.sub.3,
vitamin B.sub.5, and the like), exfoliants, retinoids (e.g.,
retinoic acid and retinol), farnesol, bisabolol, phytantriol,
glycerol, urea, guanidine (e.g., amino guanidine), clotrimazole,
ketoconazole, miconozole, griseofulvin, hydroxyzine,
diphenhydramine, pramoxine, lidocaine, procaine, mepivacaine,
monobenzone, erythromycin, tetracycline, clindamycin, meclocyline,
minocycline, hydroquinone, naproxen, ibuprofen, theophylline,
cromolyn, albuterol, topical steroids (e.g., hydrocortisone,
hydrocortisone 21-acetate, hydrocortisone 17-valerate, and
hydrocortisone 17-butyrate), betamethasone valerate, betamethasone
diproprionate, benzoyl peroxide, crotamiton, propranolol,
promethazine, and mixtures or derivatives thereof. In a preferred,
but not necessary embodiment of the present invention, the topical
composition comprises one or more skin care actives selected from
the group consisting of self-tanning agents, anti-aging agents, DNA
repair enzymes, anti-wrinkle agents, anti-acne agents,
antimicrobials, anti-inflammatory agents, skin-lightening agents,
antioxidants, proteins or peptides, vitamins and derivatives
thereof, exfoliants, and mixtures thereof.
[0028] For example, the topical or cosmetic compositions of the
present invention may include one or more antioxidants, and more
preferably one or more water-soluble extracts of biological
materials that exhibit anti-oxidant activities. If present, such
antioxidants or water-soluble extracts with anti-oxidant activities
may range from about 0.01 to 45%, preferably from about 0.05 to
20%, more preferably from about 0.1 to 15% by weight of the total
composition. Examples of suitable water-soluble extracts that
exhibit anti-oxidant activities include, but are not limited to,
extracts from: artemia, phytosphingosine, polygonum cuspidatum
root, yeast such as saccharomyces lysate, thermos thermophillus
ferment, birch (Betula alba), mimosa tenuiflora (bark) extract,
fruit, clove, rye, malt, corn, spelt, millet, barley, oat, wheat,
sesame, cumin, turmeric, green onion, celery, ginseng, ginger,
licorice, carrot, bupleurum root, Ginkgo biloba (gingko), Foeniculi
Fructus (fennel), kiwi, berry such as Morus bombycis (mulberry),
Gentiana lutea (gentian), algae such as red algae, Arctium lappa
(burdock), Salvia officinalis (sage), Lentinus edodes (shiitake
mushroom), Perilla frutescens (perilla), Filipendula Multijuga,
Fucus vesiculosis (bladderwrack, sea weed), peach kernel, Allium
sativum (garlic), Poria cocos (poria), Humulus lupulus (hops),
Mutan Cortex (Moutan Bark), Pimpinella major, Lactuca sative
(lettuce), Astragalus membranaceous (astragalus) and Rosmarinus
officinalis (rosemary), Prunus amygdalus (almond), Althea
officinale (althea), aloe, Rosae Fructus (rose fruit, or Rosa
multiflora), Scuttelaria baicalensis (Huang qin), Puerariae Radix
(Pueraria Root, or Pueraria lobata), chamomile such as Chamomillae
Flos (German chamomile), Gardenia jasminoides (zhii zi, Gardeniae
Fructus), Sophora flavescens Aiton (Sophorae Radix), chlorella,
rice bran, Paeoniae lactiflora (white peony), ziyu (Sanguisorba
officinalis, burnet), Morus alba (sang bai pi, mulberry), Glycine
max (soybean), Camellia sinensis (tea), Carthami Flos (safflower),
Aesculus hippocastanum (horse chestnut), Melissa officinalis (lemon
balm) and Coicis Semen (Coix lacryma-jobi var. ma-yuen), Angelica
keisukei, Arnica montana (arnica), Foeniculum officinale (fennel),
Isodon japonicus Hara (Isodonis Herba), Daucus Carota (carrot),
Oryza sativa (rice), Crataegus cuneata (Japanese howthorn), Acorus
calamus (sweet flag), Crataegus oxycantha (howthorn), Juniperus
communis, Ligusticum wallichii (Chinese lovage), Swertiae Herba
(Swertia Herb), Thymus vulgaris (garden thyme), Citrus reticulata
(Citrus unshiu), Capsicum tincture, Angelicae sinensis (angelica),
Aurantii Pericarpium (bitter orange peel), Ruscus aculeatus
(butcher's bloom), Vitis vinifera (grape), Tilia japonica (lime),
Citrus junos and Rosa canina (rose hip), caffeine, Cinnamomi Cortex
(cinnamon bark) and Eriobotrya japonica Lindl. (loquat), Gambir,
Echinacea, Phellodendri Cortex (amur cork tree or Phellodendron
amurense), Hypericum perforatum (St. John's wort), Citrus sinensis
(orange), Valeriana fauriei Briquet, Artemisia capillaris Thunb.,
Cucumis sativus (cucumber), Geranii Herba (Geranium Herb),
Lithospermum erythrorhizon Sieb. et Zucc., Hedera helix, Achillea
millefolium (yarrow), Ziziphus jujuba (Chinese dates), Calendula
officinalis (pot marigold), Houttuynia cordata (Houttuyniae Herba,
Houttuynia Herba), Potentilla erecta, Petroselinum crispum
(parsley), Parietaria officinalis, Santalum album (sandalwood),
Prunus persica (peach), Centaurea cyanus (cornflower), Eucalyptus
globulus (eucalyptus) and Lavandula angustifolia (lavender), Persea
americana (avocado), Nasturtium officinalis (watercress), Symphytum
officinale (comfrey), Asarum sieboldii (wild ginger), Xanthoxyum
piperitum (Japan pepper), Rehmannia glutinosa (di huang), Mentha
piperita (peppermint), Syzygium aromaticum (clove), Tussilago
farfara (coltsfoot) and Haematoxylum campechianum (logwood); Oolong
tea, Cinchona succirubra (peruvian bark), Betula verrucosa (birch)
and Glechoma hederacea (ground ivy), milk and royal jelly, honey,
cysteine and derivatives thereof, ascorbic acid and derivatives
thereof, BHA, BHT, ferulic acid and derivatives thereof, grapeseed
extract, pine bark extract, horseradish extract, hydroquinones,
rosmarinic acid, coffee robusta seed, caffeic acid, tocopherol and
derivatives thereof, green tea extract, sodium DNA, sodium
ribonucleic acid, octyl, propyl and dodecyl gallates, uric acid and
thiodiproprionate derivatives.
[0029] For another example, the topical or cosmetic compositions of
the present invention may include one or more DNA repair enzymes
and more preferably one or more DNA repair enzymes selected from
the group consisting of 8-oxoguanine DNA glucosylase,
uracil-and-hypoxanthine-DNA-glycosylase, damaged-base glycosylase
(e.g., 3-methyl-ladenine-DNA glycosylase),
3-methyladenine-DNA-glycosylase, pyrimidine dimer-specific
glycosylase, pyrimidine glycosylase/abasic lyase,
N-glycosylase/apyrimidinic lyase,
N-glycosylase/apurinic-apyrimidinic lyase, photolyase,
O.sup.6-methylguanine-DNA-methyl transferase, T4 endonuclease V,
pyrimidine dimer-specific endonuclease,
apyrimidin/apurin-endonuclease, UV damage endonuclease,
correndonuclease, and DNA exonuclease. Other DNA repair enzymes or
enzyme complexes involved in either the base excision repair (BER)
pathway, the nucleotide excision repair (NER) pathway, or the
alternative excision repair pathway can also be used for practice
of the present invention. Such DNA repair enzymes may be derived or
extracted from suitable sources, such as bacteria, algae,
protozoans, planktons, plants, and the like. Further, the DNA
repair enzymes may be encapsulated in liposomes for more efficient
delivery to the skin. Liposomes are microscopic vesicles consisting
of an aqueous core enclosed in one or more lipid layers formed by
membrane lipids, such as phospholipids and sphingomyelins.
Liposomes facilitate transfer of skin care actives into the dermis
of skin. For more details regarding encapsulation of DNA repair
enzymes in liposomes, see U.S. Pat. No. 5,296,231, the contents of
which are incorporated herein by reference in their entireties for
all purposes. If present, the DNA repair enzymes may range from
about 0.01% to 20%, preferably from about 0.1% to about 10%, and
more preferably desirably from about 0.5% to about 2%, by total
weight of the composition.
[0030] The cosmetically acceptable carrier may also contain one or
more oils, which are also known as skin conditioning agents, such
as volatile or nonvolatile silicones, esters, paraffinic
hydrocarbons, vegetable oils, and synthetic oils. Suitable volatile
or non-volatile silicones include, but are not limited to:
cyclomethicone; methyl trimethicone; octamethyltrisiloxane;
decamethyltetrasiloxane; dodecamethylpentasiloxane; dimethicone;
phenyl trimethicone trimethylsiloxyphenyl dimethicone; phenyl
dimethicone; cetyl dimethicone; dimethicone copolyol, cetyl
dimethicone copolyol; glycerolated silicones such as lauryl PEG-9
polydimethylsiloxyethyl dimethicone; or mixtures thereof. In one
embodiment, the composition may contain one or more non-volatile
silicone oils having a viscosity ranging from about 5 to 250,000
cst at 25.degree. C. Examples include dimethicone, phenyl
trimethicone, diphenyl dimethicone, and the like. Suitable esters
include mono-, di-, or triesters. Monoesters are in the general
form RCO--R' wherein R and R' are each independently a C.sub.1-45
straight or branched chain, saturated or unsaturated alkyl.
Diesters may be formed by the reaction of a C.sub.1-45 aliphatic or
aromatic mono- or dihydric alcohol with a C.sub.1-45 aliphatic or
aromatic mono- or dicarboxylic acid, as appropriate, where the
aliphatic group may be straight or branched chain, or saturated or
unsaturated. Suitable triesters include the reaction products of a
C.sub.1-45 aliphaticor aromatic alcohol having at least three
hydroxyl groups with a C.sub.1-45 carboxylic acid, or a C.sub.1-45
aliphatic or aromatic alcohol with a C.sub.1-45 tricarboxylic acid,
with the aliphatic chains being linear or branched, saturated or
unsaturated. Examples include esters of caprylic and capric acids
and glycerin such as caprylic/capric triglycerides; esters of
glycerin or polyglycerin and stearic acid such as glyceryl
stearate, diglyceryl diisostearate; esters of malic acid and
isostaryl alcohol such as diisostearyl malate; coco caprylate
caprate and the like. If present, such oils may range from about
0.1 to 99% by total weight of the composition.
[0031] The cosmetically acceptable carrier may also comprise one or
more humectants, which include, but are not limited to: glycols,
sugars, and the like. Suitable glycols are in monomeric or
polymeric form and include polyethylene and polypropylene glycols
such as PEG 4-200, which are polyethylene glycols having from 4 to
200 repeating ethylene oxide units; as well as C.sub.1-6 alkylene
glycols such as propylene glycol, butylene glycol, pentylene
glycol, and the like. Suitable sugars, some of which are also
polyhydric alcohols, are also suitable humectants. Examples of such
sugars include glucose, fructose, honey, hydrogenated honey,
inositol, maltose, mannitol, maltitol, sorbitol, sucrose, xylitol,
xylose, and so on. Preferably, the humectants used in the
composition of the invention are C.sub.1-6, preferably C.sub.2-4
alkylene glycols, most particularly butylene glycol, or glycerin.
If present, such humectants may range from about 0.001% to about
25%, preferably from about 0.005% to about 20%, more preferably
from about 0.1% to about 15%, by total weight of the topical
composition.
[0032] The cosmetically acceptable carrier may also comprise one or
more organosiloxane elastomers, generally those known as
non-emulsifying. If present, such elastomers may range from about
0.1 to 30% by weight of the total composition. Examples of suitable
elastomers include, but are not limited to dimethicone/vinyl
dimethicone crosspolymer, methylvinylsiloxanes,
methylvinylsiloxane-dimethylsiloxane copolymers,
dimethylvinylsiloxy-terminated dimethylpolysiloxanes,
dimethylvinylsiloxy-terminated
dimethylsiloxane-methylphenylsiloxane copolymers,
dimethylvinylsiloxy-terminated
dimethylsiloxane-diphenylsiloxane-methylvinylsiloxane copolymers,
trimethylsiloxy-terminated dimethylsiloxane-methylvinylsiloxane
copolymers, trimethylsiloxy-terminated
dimethylsiloxane-methylphenylsiloxane-methylvinylsiloxane
copolymers, dimethylvinylsiloxy-terminated
methyl(3,3,3-trifluoropropyl)polysiloxanes, and
dimethylvinylsiloxy-terminated
dimethylsiloxane-methyl(3,3,-trifluoropropyl)siloxane copolymers,
and the like.
[0033] The composition may also contain one or more surfactants,
particularly if present in the emulsion form. Preferably such
surfactants are nonionic and may be in the form of silicones or
organic nonionic surfactants. Suggested ranges are from about 0.1
to 40%, preferably from about 0.5 to 35%, more preferably from
about 1 to 30% by weight of the total composition. Suitable
silicone surfactants include polyorganosiloxane polymers that have
amphiphilic properties, for example contain hydrophilic radicals
and lipophilic radicals. These silicone surfactants may be liquids
or solids at room temperature. Exemplary silicone surfactants that
can be used in the present invention include, but are not limited
to: dimethicone copolyols, alkyl dimethicone copolyols, and
emulsifying silicone elastomers. Emulsifying silicone elastomers
are elastomers that have one or more hydrophilic groups such as
hydroxyl, oxyethylene, and the like bonded thereto so as to confer
hydrophilic properties to the elastomer.
[0034] Suitable organic nonionic surfactants may include
alkoxylated alcohols or ethers formed by the reaction of an alcohol
with a polyalkyleneoxide containing repeating units of alkylene
oxide. Preferably, the alcohol is a fatty alcohol having 6 to 30
carbon atoms. Examples of organic nonionic surfactants that can be
used in the present invention include, but are not limited to:
steareth 2-100, beheneth 5-30, ceteareth 2-100, ceteth 1-45, and
the like, which are formed by polyethyleneoxide with the
corresponding stearyl/behenyl/cetyl alcohol (wherein the number as
used herein designates the number of repeating units of ethylene
oxide in the polyethyleneoxide). Other alkoxylated alcohols include
esters formed by reaction of polymeric alkylene glycols with
glyceryl fatty acid, such as PEG glyceryl oleates, PEG glyceryl
stearate; or PEG polyhydroxyalkanotes such as PEG
dipolyhydroxystearate wherein the number of repeating ethylene
glycol units ranges from 3 to 1000.
[0035] Also suitable as nonionic surfactants are compounds formed
by the reaction of a carboxylic acid with an alkylene oxide or
polymeric ether. Monomeric, homopolymeric, or block copolymeric
ethers, alkoxylated sorbitan, alkoxylated sorbitan derivatives can
also be used as nonionic surfactants in the present invention.
[0036] The compositions of the invention may also contain other
ingredients such as structuring agents in the form of polymeric
structuring agents such as acrylic polymers, polyamides or
polyurethanes. The structuring agents may be water or oil soluble
or dispersible. Such structuring agents will provide structure, or
increase the viscosity of the composition. If present, suggested
ranges are from about 0.1 to 50%, preferably from about 0.5 to 40%,
more preferably from about 1 to 35% by weight of the total
composition. Suitable structuring agents include natural, synthetic
waxes, or mineral waxes such as petrolatum, candelilla, ozokerite,
synthetic wax, polyethylene, silicone waxes such as stearyl or
behenyl dimethicone, and the like. Suitable polymeric structuring
agents include carbomer, acrylic polymers or copolymers, such as
acrylates copolymer, polyacryalte-1 crosspolymer, acrylates/C10-30
alkyl acrylate crosspolymer, C10-30 alkyl acrylate crosspolymer
(e.g., those commercially available as Carbopol.RTM. or
Pemulen.RTM.), ester or amide terminated polyamides (those
commercially available from Arizona Chemical under the
Uniclear.RTM. or Sylvaclear.RTM.), or aqueous dispersions or
solutions of polyurethanes.
[0037] The topical compositions of the present invention,
especially the sunscreen compositions, are preferably
water-resistant, sweat-proof, non-irritating, non-comedogenic
(i.e., will not clog pores), and/or hypo allergenic. More
preferably, the topical compositions are transparent or
translucent, non-whitening, and can be easily absorbed into the
skin. Most preferably, the topical compositions provide maximum,
broad spectrum photoprotection and a therapeutic or curative
benefit for sun-damaged or photosensitive skin and will have an SPF
ranging from about 15 to 100, preferably from about 20 to 75.
[0038] The topical compositions of the present invention are
designed so that they may be worn daily and may be worn under
make-up. Because in one embodiment of the invention the topical
compositions of the present invention may contain relatively lower
concentrations of organic chemical sunscreen agents, they are often
perceived as more desirable to consumers who prefer sunscreens that
do not have organic sunscreen compounds in them. Preferably, the
compositions may be topically applied to any portion of the skin
that will be or will tend to be exposed to UV irradiation,
including, but not limited to, the face, the ears, the scalp, the
hands, arms, shoulders, legs, feet, abdomen and back, and any area
of the skin that an individual chooses to expose to UV, visible,
and/or IR irradiation. Such UV irradiation is typically, but not
necessarily, directed to the skin from the sun. Other UV, visible,
and IR range light sources include most typical UV light sources,
as will be appreciated by those of skill in the art, and also
including most industrial light sources.
EXAMPLES
[0039] The following examples are illustrative, but not limiting,
of the topical compositions of the present invention as described
hereinabove.
Example I
In Vitro Measurements of Photo-Protective Effect in UVB and UVA
Regions
[0040] Three (3) formulas were prepared by simply mixing the
following ingredients:
TABLE-US-00001 Concentration (wt %) Ingredients A B C De-ionized
water QS QS QS Alcohol (Denatured) 2.00 -- 2.00
Hydroxyethylcellulose 1.38 1.38 1.38 Hydroxypropyl methylcellulose
0.72 0.72 0.72 Ethylhexyl methoxycrylene ("Methoxycrylene") 2.00 --
2.00 Titanium dioxide/alginic acid/aluminum -- 4.00 4.00
hydroxide/hydrated silica
[0041] UV-absorption spectra of the above-listed three (3)
formulas, which spanned across a wavelength range of from about 290
nm to about 400 nm and covered both the UVB and UVA spectral
regions, were measured by a UV spectrophotometer commercially
available from Optometrics Corporation (Ayer, Mass.), hereinafter
referred to as the SPF-290S analyzer. Specifically, a 3M.TM.
Transpore.TM. tape was mounted onto a plastic template with a hole
of about 2.5 cm in diameter. Each formula was dotted onto the test
area of the tape (i.e., above the hole) and spread evenly to form a
sample coating layer of about 2.0 mg/cm.sup.2. The coating was
dried for about 20 minutes at room temperature. The plastic
template with the dried sample coating layer was then placed onto
the horizontal sample area of the SPF-290S analyzer, and an Atlas
Suntest XLS solar simulator manufactured by Atlas Material Testing
Solutions (Chicago, Ill.) was used as the UV source to provide UV
and near-UV radiation of from about 290 nm to 400 nm. UV absorption
spectrum of each sample coating layer was measured by the SPF-290S
analyzer, and four (4) measurements were conducted for each sample
formula and then averaged to obtain an average UV absorption curve
for each sample formula. The areas under such average UV absorption
curve in the UVB region (290 nm-320 nm) and the UVA region (320
nm-400 nm) were calculated for each sample formula and are listed
herein as follows:
TABLE-US-00002 TABLE 1 Formula UVB Absorption Area UVA Absorption
Area A 10.8 13.0 B 38.5 19.7 C 56.9 38.7
[0042] It is clear from the above table that Formula C, which
contained both Methoxycrylene and TiO.sub.2, had an UVB absorption
area (i.e., 56.9) that was greater than the sum of the UVB
absorption area measured for Formula A (i.e., 10.8) containing only
Methoxycrylene without TiO.sub.2, and the UVB absorption area
measured for Formula B (i.e., 38.5) containing only TiO.sub.2
without Methoxycrylene. Further, Formula C had an UVA absorption
area (i.e., 38.7) that was greater than the sum of the UVA
absorption area measured for Formula A (i.e., 13.0) and the UVA
absorption area measured for Formula B (i.e., 19.7). Therefore, it
seems that the combination of Methoxycrylene with TiO.sub.2
synergistically enhances the photo-protective effects of TiO.sub.2
both in the UVA and UVB regions.
Example II
[0043] Two topical sunscreen compositions containing about 3.88%
titanium dioxide and 5% zinc oxide in combination with 3%
methoxycrylene were prepared by simply mixing the following
ingredients:
TABLE-US-00003 Concentration (wt %) Ingredients Formula 3 Formula 4
De-ionized water QS QS Methyl trimethicone 12.60 12.60 Zinc oxide
5.00 5.00 C.sub.12-C.sub.15 alkyl benzoate 4.35 4.35 Isostearic
acid 0.40 0.40 Polyhydroxystearic acid 0.25 0.25 Butylene glycol
6.00 6.03 Titanium dioxide 3.88 3.88 Dimethicone 3.79 3.79
Neopentyl glycol diethylhexanoate 3.46 3.46 Beeswax 3.00 3.00
Polydiethylsiloxane 3.00 3.00 Ethylhexyl methoxycrylene
("Methoxycrylene") 3.00 3.00 Isododecane 2.18 2.18 Disteardimonium
hectorite 0.24 0.24 Propylene carbonate 0.09 0.09 Glycerin 2.00
2.00 Dimethicone/PEG-10/15 crosspolymer 0.50 0.50 Lauryl PEG-9
polydimethylsiloxyethyl 2.00 2.00 dimethicone Ethyl macadamiate
2.00 2.00 Dimethicone/vinyl dimethicone crosspolymer 0.15 0.15
Phenoxyethanol 0.83 0.83 Caprylyl glycol 0.49 0.49
Trimethylsiloxysilicate 0.33 0.33 Magnesium sulfate 1.00 1.00 Cetyl
PEG/PPG-10/1 dimethicone 1.00 1.00 Iron oxides 0.49 0.49 Xanthan
gum 0.25 0.25 Pantethine 0.16 0.16 Tocopheryl acetate 0.20 0.20
Alcaligenes polysaccharides 0.20 -- Lecithin 0.01 0.01 Hydrolyzed
wheat protein/PVP crosspolymer -- 0.40 Dipentaerythrityl
tri-polyhydroxystearate -- 2.00 Polyvinyl acetate -- 0.35
Acrylates/hydroxyesters acrylates copolymer -- 0.16 Acrylates
copolymer -- 0.30 Silicone modified acryl resin -- 0.50
Example III
[0044] Two additional topical sunscreen compositions containing
about 3.92% titanium dioxide and 5% zinc oxide in combination with
2% methoxycrylene were prepared by simply mixing the following
ingredients:
TABLE-US-00004 Concentration (wt %) Ingredients Formula 1 Formula 2
De-ionized water QS QS Methyl trimethicone 12.60 -- Butylene glycol
6.03 3.00 Zinc oxide 5.00 5.00 C.sub.12-C.sub.15 alkyl benzoate
4.35 4.35 Titanium dioxide (sunscreen grade) 3.92 3.92 Dimethicone
3.68 -- Beeswax 3.00 3.00 Polydiethylsiloxane 3.00 3.00 Neopentyl
glycol diethylhexanoate 3.00 -- Dipentaerythrityl
tri-polyhydroxystearate 2.00 0.85 Ethylhexyl methoxycrylene
("Methoxycrylene") 2.00 2.00 Glycerin 2.00 3.00 Lauryl PEG-9
polydimethylsiloxyethyl 2.00 1.00 dimethicone Ethyl macadamiate
2.00 -- Aleurites moluccana (Kukui) seed oil 2.00 -- Titanium
dioxide (pigment grade) 1.48 1.48 Cetyl PEG/PPG-10/1 dimethicone
1.00 -- Magnesium sulfate 1.00 -- Phenoxyethanol 0.83 0.31
Trioctyldodecyl citrate 0.55 0.20 Caprylyl glycol 0.49 0.47
Dimethicone/PEG-10/15 crosspolymer 0.48 -- Hydrolyzed wheat
protein/PVP crosspolymer 0.40 -- Isostearic acid 0.40 0.40 Iron
oxides 0.40 0.15 Polyvinyl acetate 0.35 -- Trimethylsiloxysilicate
0.33 -- Acrylates copolymer 0.30 -- Aluminum hydroxide 0.28 0.28
Hydrated silica 0.26 0.26 Polyhydroxystearic acid 0.25 0.25 Xanthan
gum 0.25 0.50 Tocopheryl acetate 0.20 -- Acrylates/hydroxyesters
acrylates copolymer 0.16 -- Pantethine 0.16 -- Dimethicone/vinyl
dimethicone crosspolymer 0.15 -- Alginic acid 0.06 0.06 Dipropylene
glycol 0.01 -- Lecithin 0.01 -- Tocopherol 0.01 -- Isononyl
isononanoate -- 10.00 Caprylyl methicone -- 5.00 Mica -- 5.00
Polyester-8 -- 3.00 Stearyl heptanoate -- 2.00 Steareth-21 -- 1.75
Glyceryl stearate -- 1.00 Hydrogenated lecithin -- 1.00 Magnesium
aluminum silicate -- 0.60 Cetyl alcohol -- 0.50 Trehalose -- 0.50
PEG-100 stearate -- 0.50 Steareth-2 -- 0.30 Disodium EDTA -- 0.20
Polyethylene -- 0.20 Propylene glycol dicaprate -- 0.11 Hexylene
glycol -- 0.09 Helianthus annuus (sunflower) seedcake -- 0.08
Sodium hyaluronate -- 0.02 Magnesium ascorbyl phosphate -- 0.01
Hordeum vulgare (barley) extract -- 0.01
[0045] While some illustrative embodiments of the inventions have
been described hereinabove, such illustrative embodiments should
not be interpreted in any manner to limit the broad scope of the
prevent invention. Various modifications and equivalents of the
described embodiments and components thereof will be apparent to
those of ordinary skill in the art. Some modifications and
equivalents will be readily recognized by one ordinarily skilled in
the art, while others may require no more than routine
experimentation. It is therefore understood that such modifications
and equivalents are within the spirit and scope of the present
invention.
* * * * *