U.S. patent application number 11/990490 was filed with the patent office on 2009-05-14 for cosmetic compositions comprising hydroxyfatty acids.
Invention is credited to Raphael Beumer.
Application Number | 20090124693 11/990490 |
Document ID | / |
Family ID | 37440576 |
Filed Date | 2009-05-14 |
United States Patent
Application |
20090124693 |
Kind Code |
A1 |
Beumer; Raphael |
May 14, 2009 |
Cosmetic Compositions Comprising Hydroxyfatty Acids
Abstract
The present invention is concerned with novel cosmetic or
pharmaceutical compositions. More particularly, the invention is
concerned with novel cosmetic or pharmaceutical compositions for
treating or preventing any symptoms caused by negative developments
of the physiological homeostasis of healthy skin, as well as for
the promotion of hair growth and protection from hair loss.
Inventors: |
Beumer; Raphael; (Lorrach,
DE) |
Correspondence
Address: |
NIXON & VANDERHYE, PC
901 NORTH GLEBE ROAD, 11TH FLOOR
ARLINGTON
VA
22203
US
|
Family ID: |
37440576 |
Appl. No.: |
11/990490 |
Filed: |
September 14, 2006 |
PCT Filed: |
September 14, 2006 |
PCT NO: |
PCT/EP2006/008961 |
371 Date: |
February 15, 2008 |
Current U.S.
Class: |
514/558 |
Current CPC
Class: |
A61K 31/20 20130101;
A61K 31/203 20130101; A61P 17/14 20180101; A61Q 19/00 20130101;
A61Q 7/00 20130101; A61Q 19/08 20130101; A61Q 19/007 20130101; A61Q
19/005 20130101; A61Q 19/06 20130101; A61K 8/365 20130101; A61K
31/07 20130101; A61K 8/671 20130101; A61Q 19/02 20130101; A61K
2800/75 20130101; A61P 17/04 20180101; A61P 17/00 20180101 |
Class at
Publication: |
514/558 |
International
Class: |
A61K 31/20 20060101
A61K031/20; A61P 17/00 20060101 A61P017/00 |
Foreign Application Data
Date |
Code |
Application Number |
Sep 23, 2005 |
EP |
05020779.4 |
Sep 26, 2005 |
EP |
05020905.5 |
Claims
1. A cosmetic or pharmaceutical composition comprising a fatty acid
containing 6 to 18 carbon atoms, which carries one or two hydroxy,
alkoxy, preferably methoxy or ethoxy, C2-C4-acylprotected amino,
preferably C2, or oxo group, or a salt, ester or amide of such
acids or a mixture of these acids; and a carrier conventionally
used in cosmetic or pharmaceutical compositions.
2. The composition as in claim 1, wherein the aliphatic fatty acid
is a saturated straight-chain fatty acid or .omega.-branched-chain
fatty acid.
3. The composition as in claim 2, wherein the saturated
straight-chain or .omega.-branched chain fatty acid is substituted
between the positions 6 and 12.
4. The composition as in claim 3, wherein the saturated
straight-chain or .omega.-branched fatty acid is substituted by
hydroxy.
5. The composition as in claim 4, wherein the fatty acid is
9-hydroxy stearic acid.
6. The composition as in claim 1, comprising additionally a
retinoid.
7. The composition as in claim 1, the retinoid is retinoic acid or
a derivative thereof.
8. The composition as in claim 1, wherein the retinoid is retinyl
acetate, phenylbutyrate, propionate, octanoate, laurate, palmitate,
oleate, linoleate; retinyl alkyl carbonate;
retinoxytrimethylsilane; (all trans)-retinal or its acetals; or
methoxy PEG-12 retinamide.
9. The composition according to claim 1, wherein the amount of the
fatty acid is from about 0.0001 to about 50% by weight of the total
composition.
10. The composition according to claim 1, wherein the amount of the
fatty acid is from about 0.001 to about 20% by weight of the total
composition.
11. The composition according to claim 1, wherein the amount of the
compound of the fatty acid is from about 0.01 to about 1% by weight
of the total composition.
12. The composition according to claim 6, wherein the amount of the
retinoid or derivative thereof is from about 0.001 to about 50% by
weight of the total composition.
13. The composition according to claim 6, wherein the amount of the
retinoid or derivative thereof is from about 0.001 to about 20% by
weight of the total composition.
14. The composition according to claim 6, wherein the amount of the
retinoid or derivative thereof is from about 0.01 to about 1% by
weight of the total composition.
15. The composition according to claim 6, wherein the ratio of the
fatty acid to the retinoid or derivative thereof is from about
1000:1 to about 1:1000 by weight.
16. The composition according to claim 6, wherein the ratio of the
fatty acid to the retinoid or derivative thereof is from about
100:1 to about 1:100 by weight.
17. The composition according to claim 6, wherein the ratio of the
fatty acid to the retinoid or derivative thereof is from about 30:1
to about 1:30 by weight.
18. A composition as in claim 1, which is for prevention or
treatment of symptoms caused by negative developments of the
physiological homeostasis of healthy skin, promotion of hair
growth, protection from hair loss, prevention and treatment of
itchy or irritated skin.
19. A composition as in claim 1, which is for the prevention or
treatment of pigmentation disorders and/or for providing an even
skin tone.
20. A composition as in claim 1, which is for fortifying the
pigmentation by enhancing the effect of a tanning active.
21. A composition as in claim 1, which is for the treatment or
prevention of wrinkles or dry skin or sensitive skin, for the
promotion of hair growth, for the protection from hair loss, and
for thickening the epidermis.
22. A method of treatment or prevention of symptoms caused by
negative developments of the physiological homeostasis of healthy
skin as well as treatment or prevention of itchy or irritated skin
and of promotion of hair growth and of protection from hair loss,
which method comprises the step of topically administering to a
person in need of such treatment or prevention an effective amount
of a fatty acid or a salt, ester or amide, optionally in
combination with a retinoid.
Description
[0001] The present invention is concerned with novel cosmetic or
pharmaceutical compositions. More particularly, the invention is
concerned with novel cosmetic or pharmaceutical compositions for
treating or preventing any symptoms caused by negative developments
of the physiological homeostasis of healthy skin, as well as for
the promotion of hair growth and protection from hair loss.
[0002] Thus, in one aspect, the present invention is concerned with
cosmetic or pharmaceutical compositions comprising a fatty acid
containing 6 to 18 carbon atoms, which carries one or two hydroxyl,
alkoxy, preferably methoxy or ethoxy, C2-C4-acylprotected amino,
preferably C2, or oxo group, preferably between the positions C6
and C12; or a salt, ester or amide of such acids or a mixture of
these acids; and a carrier conventionally used in cosmetic or
pharmaceutical compositions.
[0003] The ester or amide are, preferably, an alkyl ester or alkyl
amide, wherein the term "alkyl" encompasses straight chain as well
as branched alkyl groups, i.e. that "C.sub.1-4-alkyl" encompasses
straight chain C.sub.1-4-alkyl (methyl, ethyl, n-propyl, n-butyl)
as well as branched C.sub.3-4-alkyl (iso-propyl, iso-butyl,
tert-butyl).
[0004] The salt may by formed by any cosmetically acceptable cation
which means any metal cation as well as any organic cation that is
not toxic to the skin and/or does not cause allergic reactions.
Examples of such cations are ammonium salts and alkyl ammonium
salts, alkali cations such as sodium and potassium ions and
alkaline earth metal cations such as calcium und magnesium
ions.
[0005] In one embodiment of the present invention the aliphatic
fatty acid is a saturated straight-chain fatty acid or
.omega.-branched-chain fatty acid which preferably has 6 to 18
carbon atoms. In another embodiment the aliphatic fatty acid is a
saturated straight-chain or .omega.-branched chain fatty acid which
has 6 to 18 carbon atoms and is substituted, preferably by hydroxy,
between the positions C6 and C12. A particularly preferred fatty
acid is 9-hydroxy stearic acid.
[0006] In a further aspect, the invention is concerned with
cosmetic or pharmaceutical compositions comprising a fatty acid or
a salt, ester or amide with the definitions and preferences as
given above, and a retinoid.
[0007] Retinoids for use in the invention are, e.g., retinoic acid
or retinol and isomers, e.g. 9-, 11- or 13-cis isomers thereof, and
derivatives thereof which comprise retinyl esters such as the
acetate, phenylbutyrate, propanoate, laurate, palmitate, oleate,
linoleate; or retinyl alkyl carbonate; or ethers such as
retinoxytrimethylsilane; or (all trans)-retinal or its acetals; or
retinoic acid or amides thereof such as methoxy PEG-12 retinamide
("PEG-12"=--(CH.sub.2--CH.sub.2--O--).sub.12).
[0008] More specifically, the invention is concerned with cosmetic
or pharmaceutical compositions comprising at least one fatty acid
or a salt, ester or amide with the definitions and preferences as
given above, and optionally one retinoid, for the treatment or
prevention of symptoms caused by negative developments of the
physiological homeostasis of healthy skin, as well as for the
promotion of hair growth and protection from hair loss.
[0009] Treatment or prevention of symptoms caused by negative
developments of the physiological homeostasis of healthy skin
comprises treatment or prevention of wrinkles or dry skin or
sensitive skin, thickening of the epidermis, inhibition of
senescence of skin cells, prevention or treatment of photodamage,
prevention or treatment of oxidative stress phenomena, prevention
or treatment of cellulite, prevention and treatment of disturbances
in ceramide and lipid synthesis, prevention of excess sebum
production, reduction of activities of matrix metallo proteases or
other proteases in the skin, treatment and prevention of
inflammatory skin conditions including acne (=anti-acne), atopic
eczema, polymorphic light eruption, psoriasis and vertiligo.
[0010] In still another aspect, the invention is concerned with a
method of treatment or prevention of symptoms caused by negative
developments of the physiological homeostasis of healthy skin as
well as treatment or prevention of itchy or irritated skin and of
promotion of hair growth and of protection from hair loss which
method provides topically administering to a person in need of such
treatment or prevention an effective amount of a fatty acid or a
salt, ester or amide with the definitions and preferences as given
above, optionally and preferably in combination with a retinoid and
preferably in the form of a cosmetic or pharmaceutical composition
according to the invention.
[0011] A preferred embodiment of the present invention is a method
of treating or preventing wrinkles or human dry skin or sensitive
skin, of promoting hair growth, of protecting from hair loss and of
thickening the epidermis, which method comprises the step of
topically administering to a person in need of such treatment or
prevention an effective amount of a fatty acid or a salt, ester or
amide with the definitions and preferences as given above,
optionally and preferably in combination with a retinoid.
[0012] A further object of the present invention is a method for
the prevention or treatment of pigmentation disorders and/or for
providing an even skin tone, which method comprises the step of
topically administering to a person in need of such prevention or
treatment an effective amount of a composition according to the
present invention as defined above, wherein the composition
contains a retinoid.
[0013] Another object of the present invention is a method for
fortifying the pigmentation which method comprises the step of
topically administering to a person in need of such fortification
an effective amount of a composition according to the present
invention as defined above and topically administering a tanning
active, wherein the tanning active may be administered before,
after or simultaneously with the administration of the effective
amount of the composition according to the present invention, and
wherein any retinoid is essentially absent in such a
composition.
[0014] The term `an effective amount` refers to an amount necessary
to obtain a physiological effect. The physiological effect may be
achieved by one application dose or by repeated applications. The
dosage administered may, of course, vary depending upon known
factors, such as the physiological characteristics of the
particular composition comprising the fatty acid or a salt, ester
or amide with the definitions and preferences as given above,
optionally in combination with a retinoid and its mode and route of
administration; the age, health and weight of the recipient; the
nature and extent of the symptoms; the kind of concurrent
treatment; the frequency of treatment; and the effect desired and
can be adjusted by a person skilled in the art.
[0015] In another embodiment, the compositions according to the
present invention can be used for the treatment or prevention of
symptoms caused by negative developments of the physiological
homeostasis of healthy skin as defined above, as well as for the
promotion of hair growth and protection from hair loss. The
compositions according to the present invention can further be used
for the treatment or prevention of itchy or irritated skin or for
fortifying the pigmentation (the latter, however, only, if no
retinoid but a tanning active is present.). If retinoid is,
however, present in the composition of this invention the
composition can be used for the prevention or treatment of
pigmentation disorders and/or for providing an even skin tone,
since the boosting of retinoids by the fatty acids or a salt, ester
or amide thereof as defined above may lead to a depigmentation.
[0016] Preferably the compositions of the present invention are
used for the treatment or prevention of wrinkles or dry skin or
sensitive skin, for the promotion of hair growth, for the
protection from hair loss, for thickening the epidermis, (if
retinoid is present) for the prevention or treatment of
pigmentation disorders and/or for providing an even skin tone,
and/or (if retinoid is absent and a tanning active is present) for
fortifying the pigmentation. Thus the composition according to the
present invention, i.e. the fatty acids or a salt, ester or amide
thereof with the definitions and preferences as defined above may
fortify the pigmentation by enhancing the effect of a tanning
active.
[0017] While, typically, the cosmetic or pharmaceutical
compositions according to the present invention contain one of the
fatty acids as defined above, the invention is not limited to that
particular aspect and two or more fatty acids or a salt, ester or
amide thereof as defined above may be present. As stated above, a
retinoid may be additionally present, providing an additive or
synergistic cosmetic effect, i.e. an improvement or prevention of
symptoms caused by negative developments of the physiological
homeostasis of healthy skin, as well as promotion of hair growth
and protection from hair loss. Again, two or more retinoids may be
present. If a retinoid is present in the compositions of the
present invention, the ratio of the fatty acid or a salt, ester or
amide with the definitions and preferences as given above) to the
retinoid is suitably from about 1000:1 to 1:1000, more preferably
from about 100:1 to 1:100 and in particular from about 30:1 to 1:30
by weight. The fatty acids or a salt, ester or amide thereof as
defined above show also an additive or synergistic effect with
retinoids which are already present in the human skin.
[0018] In the compositions provided by the present invention, the
amount of the fatty acid or a salt, ester or amide with the
definitions and preferences as given above is suitably from about
0.0001 to about 50%, preferably from about 0.001 to about 20% by
weight of the total composition. More preferably, the fatty acid as
defined above are contained in the composition in an amount of
about 0.01% by weight to about 1% by weight, most preferably in an
amount of about 0.5% by weight. If a retinoid or derivative thereof
is present, the amount of the latter is suitably from about 0.0001
to about 50% by weight, preferably from about 0.001 to about 20% by
weight, most preferably in an amount of about 0.01 to about 1
weight %, in particular in an amount of about 0.1% by weight, based
on the total amount of the composition. Preferred according to the
invention is a composition comprising the fatty acid or a salt,
ester or amide with the definitions and preferences as given above
in an amount of about 0.5% by weight and a retinoid or derivative
thereof in an amount of about 0.1% by weight, based on the total
amount of the composition.
[0019] The term "cosmetic composition" as used herein e.g. refers
to topical compositions for care of the human skin, see also the
heading "Kosmetika" in Rompp Lexikon Chemie, 10th edition 1997,
Georg Thieme Verlag Stuttgart, New York.
[0020] Regarding the kind of the topical (cosmetic or
pharmaceutical) compositions and the preparation of the topical
compositions as well as for further suitable additives, it can be
referred to the pertinent literature, e.g. to Novak G. A., Die
kosmetischen Praparate--Band 2, Die kosmetischen
Praparate--Rezeptur, Rohstoffe, wissenschaftliche Grundlagen
(Verlag fur Chem. Industrie H. Ziolkowski K G, Augsburg).
[0021] The amount of the cosmetic or pharmaceutical composition
according to the invention, which is to be applied to the skin
depends on the concentration of the active ingredients in the
compositions and the desired cosmetic or pharmaceutical effect. For
example, application can be such that a creme is applied to the
skin. A creme is usually applied in an amount of 2 mg
creme/cm.sup.2 skin. The amount of the composition which is applied
to the skin is, however, not critical, and if with a certain amount
of applied composition the desired effect cannot be achieved, a
higher concentration of the active ingredients can be used e.g. by
applying more of the composition or by applying compositions which
contain more active ingredient.
[0022] The cosmetic or pharmaceutical composition according to the
invention is preferably applied at least once per day, e.g. twice
or three times a day. Usually it takes at least two weeks until the
desired effect is achieved. However, it can take several weeks or
even months until the desired effect is fully maximized.
[0023] The compositions of the present invention contain the fatty
acids or a salt, ester or amide thereof with the definitions and
preferences as defined above with cosmetically or pharmaceutically
acceptable excipients or diluents. If nothing else is stated, the
excipients, additives, diluents, etc. mentioned in the following
are suitable for cosmetic compositions.
[0024] If nothing else is stated, in this application parts and
percentages are per weight and are based on the total weight of the
composition.
[0025] Preferably, the cosmetic or pharmaceutical compositions of
the present invention are topical compositions in the form of a
suspension or dispersion in solvents or fatty substances, or
alternatively in the form of an emulsion or micro emulsion (in
particular of O/W or W/O type, O/W/O or W/O/W-type), PET-emulsions,
multiple emulsions, bickering emulsions, hydrogels, alcoholic gels,
lipogels, one or multiphase solutions or a vesicular dispersion and
other usual compositions, which can also be applied by pens, as
masks or as sprays. The emulsions can also contain anionic,
nonionic, cationic or amphoteric surfactant(s).
[0026] Preferred compositions according to the invention are skin
care preparations, hair-care preparations, decorative preparations,
light protection preparations and functional preparations.
[0027] Examples of skin care preparations are, in particular, body
oils, body lotions, body gels, treatment creams, skin protection
ointments, shaving preparations, such as shaving foams or gels,
skin powders such as baby powder, moisturizing gels, moisturizing
sprays, revitalizing body sprays, cellulite gels, anti acne
preparations and peeling preparations.
[0028] Examples of hair care preparations are, for example,
hair-washing preparations in the form of shampoos, hair
conditioners, hair-care preparations, e.g. treatment preparations,
pre-treatment preparations, hair tonics, styling creams, styling
gels, pomades, hair rinses, treatment packs, intensive hair
treatments, hair-straightening preparations, liquid hair-setting
preparations, hair foams and hairsprays and lacquers, perming
agents, hair gels, hair fixatives and hair dying or bleaching
agents.
[0029] Examples of decorative preparations are in particular
lipstick, eye shadow, mascaras, dry and moist make-up, rouge,
powders, and suntan lotions.
[0030] Examples of functional preparations are cosmetic or
pharmaceutical compositions containing active ingredients such as
hormone preparations, vitamin preparations, vegetable extract
preparations, anti-ageing preparations, and antimicrobial
(antibacterial or antifungal) preparations without being limited
thereto.
[0031] Cosmetic compositions in accordance with the invention can
be in the form of a liquid, a lotion, a thickened lotion, a gel, a
cream, a milk, an ointment, a paste, a powder, a make-up, or a
solid tube stick and can be optionally be packaged as an aerosol
and can be provided in the form of a mousse such as a aerosol
mousse, a foam or a spray foams, sprays, sticks, a gel, a plaster,
a powder, a cleanser, a soap or aerosols or wipes.
[0032] The compositions of the invention can also contain usual
cosmetic or pharmaceutical adjuvants and additives, such as
preservatives/antioxidants, fatty substances/oils, water, organic
solvents, silicones, thickeners, softeners, emulsifiers,
sunscreens, antifoaming agents, moisturizers, fragrances,
surfactants, fillers, sequestering agents, anionic, cationic,
nonionic or amphoteric polymers or mixtures thereof, propellants,
acidifying or basifying agents, dyes, colorants, pigments or
nanopigments, e.g. those suited for providing a photoprotective
effect by physically blocking out ultraviolet radiation, or any
other ingredients usually formulated into cosmetics or
medicaments.
[0033] An additional amount of antioxidants/preservatives is
generally preferred. Based on the invention all known antioxidants
usually formulated into cosmetics or medicaments can be used.
Especially preferred are antioxidants chosen from the group
consisting of amino acids (e.g. glycine, histidine, tyrosine,
tryptophane) and their derivatives, imidazole (e.g. urocanic acid)
and derivatives, peptides such as D,L-carnosine, D-carnosine,
L-carnosine and derivatives (e.g. anserine), carotenoids, carotenes
(e.g. .alpha.-carotene, .beta.-carotene, lycopene) and derivatives,
chlorogenic acid and derivatives, lipoic acid and derivatives (e.g.
dihydrolipoic acid), aurothioglucose, propylthiouracil and other
thiols (e.g. thioredoxine, glutathione, cysteine, cystine,
cystamine and its glycosyl-, N-acetyl-, methyl-, ethyl-, propyl-,
amyl-, butyl- and lauryl-, palmitoyl-; oleyl-, .gamma.-linoleyl-,
cholesteryl- and glycerylester) and the salts thereof,
dilaurylthiodipropionate, distearylthiodipropionate,
thiodipropionic acid and its derivatives (ester, ether, peptides,
lipids, nucleotides, nucleosides and salts) as well as sulfoximine
compounds (such as buthioninsulfoximine, homocysteinsulfoximine,
buthioninsulfone, penta-, hexa-, heptathioninsulfoximine) in very
low compatible doses (e.g. pmol to .mu.mol/kg), additionally
(metal)-chelators (such as .alpha.-hydroxyfatty acids, palmic-,
phytinic acid, lactoferrin), .beta.-hydroxyacids (such as citric
acid, lactic acid, malic acid), huminic acid, gallic acid, gallic
extracts, bilirubin, biliverdin, EDTA, EGTA and its derivatives,
unsaturated fatty acids and their derivatives (such as
.gamma.-linoleic acid, linolic acid, oleic acid), folic acid and
its derivatives, ubiquinone and ubiquinol and their derivatives,
vitamin C and derivatives (such as ascorbylpalmitate and
ascorbyltetraisopalmitate, Mg-ascorbylphosphate,
Na-ascorbylphosphate, Na-ascorbylacetate), tocopherol and
derivatives (such as vitamin-E-acetate), mixtures of natural or
synthetic vitamin E, vitamin A and derivatives (vitamin-A-palmitate
and -acetate) as well as coniferylbenzoat, rutinic acid and
derivatives, .alpha.-glucosylrutin, ferulic acid,
furfurylidenglucitol, carnosine, butylhydroxytoluene,
butylhydroxyanisole, trihydroxybutylrophenone, urea and its
derivatives, mannose and derivatives, zinc and derivatives (e.g.
ZnO, ZnSO.sub.4), selenium and derivatives (e.g. selenomethionine),
stilbenes and derivatives (such as stilbenoxide,
trans-stilbenoxide) and suitable derivatives (salts, esters,
ethers, sugars, nucleotides, nucleosides, peptides and lipids) of
the named active ingredients. One or more
pre-servativeslantioxidants may be present in an amount about 0.01
weight % to about 10 weight % of the total weight of the
composition of the present invention. Preferably, one or more
preservatives/antioxidants are present in an amount about 0.1
weight % to about 1 weight %.
[0034] Typically topical formulations also contain surface active
ingredients like emulsifiers, solubilizers and the like. An
emulsifier enables two or more immiscible components to be combined
homogeneously. Moreover, the emulsifier acts to stabilize the
composition. Emulsifiers that may be used in the present invention
in order to form O/W, W/O, O/W/O or W/O/W emulsions/microemulsions
include sorbitan oleate, sorbitan sesquioleate, sorbitan
isostearate, sorbitan trioleate, polyglyceryl-3-diisostearate,
polyglycerol esters of oleic/isostearic acid, polyglyceryl-6
hexaricinolate, polyglyceryl-4-oleate, polyglyceryl-4 oleate/PEG-8
propylene glycol cocoate, oleamide DEA, TEA myristate, TEA
stearate, magnesium stearate, sodium stearate, potassium laurate,
potassium ricinoleate, sodium cocoate, sodium tallowate, potassium
castorate, sodium oleate, and mixtures thereof. Further suitable
emulsifiers are phosphate esters and the salts thereof such as
cetyl phosphate (Amphisol.RTM. A), diethanolamine cetyl phosphate
(Amphisol.RTM.), potassium cetyl phosphate (Amphisol.RTM. K),
sodium glyceryl oleate phosphate, hydrogenated vegetable glyceride
phosphates and mixtures thereof. Furthermore, one or more synthetic
polymers may be used as an emulsifier. For example, PVP eicosene
copolymer, acrylates/C.sub.10-30 alkyl acrylate crosspolymer,
acrylates/steareth-20 methacrylate copolymer, PEG-22/dodecyl glycol
copolymer, PEG-45/dodecyl glycol copolymer, and mixtures thereof.
The preferred emulsifiers are cetyl phosphate (Amphisol.RTM. A),
diethanolamine cetyl phosphate (Amphisol.RTM.), potassium cetyl
phosphate (Amphisol.RTM. K), PVP Eicosene copolymer,
acrylates/C.sub.10-30-alkyl acrylate crosspolymer, PEG-20 sorbitan
isostearate, sorbitan isostearate, and mixtures thereof. The one or
more emulsifiers are present in a total amount about 0.01 weight %
to about 20 weight % of the total weight of the composition of the
present invention. Preferably, about 0.1 weight % to about 10
weight % of emulsifiers is used.
[0035] The lipid phase of the topical compositions can
advantageously be chosen from:
[0036] mineral oils and mineral waxes;
[0037] oils such as triglycerides of caprinic acid or caprylic acid
and castor oil;
[0038] oils or waxes and other natural or synthetic oils, in a
preferred embodiment esters of fatty acids with alcohols e.g.
isopropanol, propylene glycol, glycerin or esters of fatty alcohols
with carboxylic acids or fatty acids;
[0039] alkylbenzoates; and/or
[0040] silicone oils such as dimethylpolysiloxane,
diethylpolysiloxane, diphenylpolysiloxane, cyclomethicones and
mixtures thereof.
[0041] Exemplary fatty substances which can be incorporated in the
oil phase of the emulsion, microemulsion, oleo gel, hydrodispersion
or lipodispersion of the present invention are advantageously
chosen from esters of saturated and/or unsaturated, linear or
branched alkyl carboxylic acids with 3 to 30 carbon atoms, and
saturated and/or unsaturated, linear and/or branched alcohols with
3 to 30 carbon atoms as well as esters of aromatic carboxylic acids
and of saturated and/or unsaturated, linear or branched alcohols of
3-30 carbon atoms. Such esters can advantageously be selected from
octylpalmitate, octylcocoate, octylisostearate,
octyldodecylmyristate, cetearylisononanoate, isopropylmyristate,
isopropylpalmitate, isopropylstearate, isopropyloleate,
n-butylstearate, n-hexyllaureate, n-decyloleat, isooctylstearate,
isononylstearate, isononylisononanoate, 2-ethyl hexylpalmitate,
2-ethylhexyllaurate, 2-hexyldecylstearate, 2-octyldodecylpalmitate,
stearylheptanoate, oleyloleate, oleylerucate, erucyloleate,
erucylerucate, tridecylstearate, tridecyltrimellitate, as well as
synthetic, half-synthetic or natural mixtures of such esters e.g.
jojoba oil.
[0042] Other fatty components suitable for use in the topical
compositions of the present invention include polar oils such as
lecithines and fatty acid triglycerides, namely triglyceryl esters
of saturated and/or unsaturated, straight or branched carboxylic
acid with 8 to 24 carbon atoms, preferably of 12 to 18 carbon-atoms
whereas the fatty acid triglycerides are preferably chosen from
synthetic, half synthetic or natural oils (e.g. cocoglyceride,
olive oil, sun flower oil, soybean oil, peanut oil, rape seed oil,
sweet almond oil, palm oil, coconut oil, castor oil, hydrogenated
castor oil, wheat oil, grape seed oil, macadamia nut oil and
others); apolar oils such as linear and/or branched hydrocarbons
and waxes e.g. mineral oils, Vaseline (petrolatum); paraffins,
squalane and squalene, polyolefines, hydrogenated polyisobutenes
and isohexadecanes, favored polyolefines are polydecenes; dialkyl
ethers such as dicaprylylether; linear or cyclic silicone oils such
as preferably cyclomethicones (octamethylcyclotetrasiloxane;
cetyldimethicone, hexamethylcyclotrisiloxane, polydimethylsiloxane,
poly(methylphenylsiloxane) and mixtures thereof.
[0043] Still other fatty components which can advantageously be
incorporated in topical compositions of the present invention are
isoeikosane; neopentylglykoldiheptanoate;
propyleneglykoldicaprylate/dicaprate;
caprylic/capric/diglycerylsuccinate; butyleneglycol
caprylatlcaprat; C.sub.12-13-alkyllactate; di-C.sub.12-13
alkyltartrate; triisostearin; dipentaerythrityl
hexacaprylat/hexacaprate; propylenglycolmonoisostearate;
tricaprylin; dimethylisosorbid. Especially beneficial is the use of
mixtures C.sub.12-15-alkylbenzoate and 2-ethylhexylisostearate,
mixtures C.sub.12-15-alkylbenzoate and isotridecylisononanoate as
well as mixtures of C.sub.12-15-alkylbenzoate,
2-ethylhexylisostearate and isotridecylisononanoate.
[0044] The oily phase of the compositions of the present invention
can also contain natural vegetable or animal waxes such as bee wax,
china wax, bumblebee wax and other waxes of insects as well as shea
butter and cocoa butter.
[0045] A moisturizing agent may be incorporated into a topical
composition of the present invention to maintain hydration or
rehydrate the skin. Moisturizers that prevent water from
evaporating from the skin by providing a protective coating are
called emollients.
[0046] Additionally an emollient provides a softening or soothing
effect on the skin surface and is generally considered safe for
topical use. Preferred emollients include mineral oils, lanolin,
petrolatum, capric/caprylic triglyceraldehydes, cholesterol,
silicones such as dimethicone, cyclomethicone, almond oil, jojoba
oil, avocado oil, castor oil, sesame oil, sunflower oil, coconut
oil and grape seed oil, cocoa butter, olive oil aloe extracts,
fatty acids such as oleic and stearic, fatty alcohols such as cetyl
and hexadecyl (ENJAY), diisopropyl adipate, hydroxybenzoate esters,
benzoic acid esters of C.sub.9-15-alcohols, isononyl iso-nonanoate,
ethers such as polyoxypropylene butyl ethers and polyoxypropylene
cetyl ethers, and C.sub.12-15-alkyl benzoates, and mixtures
thereof. The most preferred emollients are hydroxybenzoate esters,
aloe vera, C.sub.12-15-alkyl benzoates, and mixtures thereof. An
emollient is present in an amount of about 1 weight % to about 20
weight % of the total weight of the composition. The preferred
amount of emollient is about 2 weight % to about 15 weight %, and
most preferably about 4 weight % to about 10 weight %.
[0047] Moisturizers that bind water, thereby retaining it on the
skin surface are called humectants. Suitable humectants can be
incorporated into a topical composition of the present invention
such as glycerin, polypropylene glycol, polyethylene glycol, lactic
acid, pyrrolidone carboxylic acid, urea, phospholipids, collagen,
elastin, ceramides, lecithin sorbitol, PEG-4, and mixtures thereof.
Additional suitable moisturizers are polymeric moisturizers of the
family of water soluble and/or swellable/and/or with water gelating
polysaccharides such as hyaluronic acid, chitosan and/or a fucose
rich polysaccharide which is e.g. available as Fucogel.RTM.1000
(CAS-Nr. 178463-23-5) by SOLABIA S. One or more humectants are
optionally present at about 0.5 weight % to about 8 weight % in a
composition of the present invention, preferably about 1 weight %
to about 5 weight %.
[0048] The aqueous phase of the preferred topical compositions of
the present invention can contain the usual cosmetic or
pharmaceutical additives such as alcohols, especially lower
alcohols, preferably ethanol and/or isopropanol, low diols or
polyols and their ethers, preferably propyleneglycol, glycerin,
ethyleneglycol, ethyleneglycol monoethyl- or monobutylether,
propyleneglycol monomethyl- or -monoethyl- or -monobutylether,
diethyleneglycol monomethyl- or monoethylether and analogue
products, polymers, foam stabilisators; electrolytes and especially
one or more thickeners.
[0049] Thickeners that may be used in formulations of the present
invention to assist in making the consistency of a product suitable
include carbomer, siliciumdioxide, magnesium and/or aluminium
silicates, beeswax, stearic acid, stearyl alcohol polysaccharides
and their derivatives such as xanthan gum, hydroxypropyl cellulose,
polyacrylamides, acrylate crosspolymers preferably a carbomer, such
as Carbopole.RTM. of type 980, 981, 1382, 2984, 5984 alone or
mixtures thereof.
[0050] Suitable neutralizing agents which may be included in the
composition of the present invention to neutralize components such
as e.g. an emulsifier or a foam builder/stabilizer include but are
not limited to alkali hydroxides such as a sodium and potassium
hydroxide; organic bases such as diethanolamine (DEA),
triethanolamine (TEA), aminomethyl propanol, and mixtures thereof;
amino acids such as arginine and lysine and any combination of any
foregoing. The neutralizing agent can be present in an amount of
about 0.01 weight % to about 8 weight % in the composition of the
present invention, preferably, 1 weight % to about 5 weight %.
[0051] The addition of electrolytes into the composition of the
present invention may be necessary to change the behavior of a
hydrophobic emulsifier. Thus, the emulsions/microemulsions of this
invention may contain preferably electrolytes of one or several
salts including anions such as chloride, sulfates, carbonate,
borate and aluminate, without being limited thereto. Other suitable
electrolytes can be on the basis of organic anions such as, but not
limited to, lactate, acetate, benzoate, propionate, tartrate and
citrate. As cations preferably ammonium, alkylammonium, alkali- or
alkaline earth metals, magnesium-, iron- or zinc-ions are selected.
Especially preferred salts are potassium and sodium chloride,
magnesium sulfate, zinc sulfate and mixtures thereof. Electrolytes
can be present in an amount of about 0.01 weight % to about 8
weight % in the composition of the present invention.
[0052] According to the invention for preparing the compositions of
the invention the active ingredients can be used as such or in an
encapsulated form, for example in a liposomal form. Liposomes are
preferably formed with lecithins with or without addition of
sterols or phytosterols. The encapsulation of the active
ingredients can be alone or together with other active ingredients.
It is possible to encapsulate only the fatty acid or a salt, ester
or amide thereof with the preferences and definitions as defined
above or only the retinoid, but it is also possible to encapsulate
both ingredients either together or in separate capsules.
[0053] Other embodiments include solid or semisolid capsules aiming
to protect the retinoid from degradation or for controlled
delivery. The capsule may contain the retinoid alone or together
with the fatty acid or a salt, ester or amide thereof with the
preferences and definitions as defined above. Suitable
encapsulation technologies are for example described in WO 0180823,
WO 9903450, WO 9317784 or in Fragrance Journal (2001), 29(2),
83-90.
[0054] The composition of the present invention can also contain
one or more additional pharmaceutically or cosmetically active
ingredients, in particular for preventing or reducing acne,
wrinkles, lines, atrophy, inflammation, as well as topical
anesthetics, artificial tanning agents and accelerators,
antimicrobial agents, antifungal agents and sun screening additives
without being limited thereto.
[0055] Examples of such ingredients are peptides (e.g.,
Matrixyl.TM.[pentapeptide derivative]), oligopeptides, wax-based
synthetic peptides (e.g., octyl palmitate and tribehenin and
sorbitan isostearate and palmitoyl-oligopeptide), glycerol, urea,
guanidine (e.g. amino guanidine); vitamins and derivatives thereof
such as vitamin C (ascorbic acid), vitamin A (e.g., retinoid
derivatives such as retinyl palmitate or retinyl propionate),
vitamin E (e.g., tocopherol acetate), vitamin B.sub.3 (e.g.
niacinamide) and vitamin B.sub.5 (e.g. panthenol), vitamin B.sub.6
and vitamin B.sub.12, biotin, folic acid; anti-acne actives or
medicaments (e.g. resorcinol, salicylic acid, and the like);
antioxidants (e.g. phytosterols, lipoic acid); flavonoids (e.g.
isoflavones, phytoestrogens); skin soothing and healing agents such
as aloe vera extract, allantoin and the like; agents suitable for
aesthetic purposes such as essential oils, fragrances, skin
sensates, opacifiers, aromatic compounds (e.g., clove oil, menthol,
camphor, eucalyptus oil, and eugenol), desquamatory actives,
hydroxy acids such as AHA acids, radical scavengers, farnesol,
antifungal actives in particular bisabolol, alkyldiols such as
1,2-pentanediol, hexanediol or 1,2-octanediol, phytol, polyols such
as phytanetriol, ceramides and pseudoceramides, amino acids,
protein hydrolysates, polyunsaturated fatty acids, plant extracts
like kinetin, DNA or RNA and their fragmentation products,
carbohydrates, conjugated fatty acids, carnitin, carnosine,
biochinonen, phytofluen, phytoen, and their corresponding
derivatives.
[0056] Additionally the cosmetic and pharmaceutical topical
composition of the present invention may contain UV-screening
agents (UV-filter). The additional UV-screening agents are
advantageously selected from IR, UV-A, UV-B, UV-C and/or broadband
filters. Examples of UV-B or broad spectrum screening agents, i.e.
substances having absorption maximums between about 290 nm and 340
nm may be organic or inorganic compounds. Organic UV-B or broadband
screening agents are e.g. acrylates such as 2-ethylhexyl
2-cyano-3,3-diphenylacrylate (octocrylene, PARSOL.RTM. 340), ethyl
2-cyano-3,3-diphenylacrylate and the like; camphor derivatives such
as 4-methyl benzylidene camphor (PARSOL.RTM. 5000), 3-benzylidene
camphor, camphor benzalkonium methosulfate, polyacrylamidomethyl
benzylidene camphor, sulfo benzylidene camphor, sulphomethyl
benzylidene camphor, therephthalidene dicamphor sulfonic acid and
the like; Cinnamate derivatives such as ethylhexyl methoxycinnamate
(PARSOL.RTM. MCX), ethoxyethyl methoxycinnamate, diethanolamine
methoxycinnamate (PARSOL.RTM. Hydro), isoamyl methoxycinnamate and
the like as well as cinnamic acid derivatives bond to siloxanes;
p-aminobenzoic acid derivatives, such as p-aminobenzoic acid,
2-ethylhexyl p-dimethylaminobenzoate, N-oxypropylenated ethyl
p-aminobenzoate, glyceryl p-aminobenzoate; benzophenones such as
benzophenone-3, benzophenone-4,
2,2',4,4'-tetrahydroxy-benzophenone,
2,2'-dihydroxy-4,4'-dimethoxybenzophenone and the like; esters of
benzalmalonic acid such as di-(2-ethylhexyl)
4-methoxybenzalmalonate; esters of
2-(4-ethoxy-anilinomethylene)propandioic acid such as 2-(4-ethoxy
anilinomethylene) propandioic acid diethyl ester as described in
the European Patent Publication EP 0895 776; organosiloxane
compounds containing benzmalonate groups as described in the
European Patent Publications EP 0358584 B1, EP 0538431 B1 and EP
0709080 A1 such as PARSOL.RTM. SLX; drometrizole trisiloxane
(Mexoryl XL); imidazole derivatives such as e.g. 2-phenyl
benzimidazole sulfonic acid and its salts (PARSOL.RTM.HS). Salts of
2-phenyl benzimidazole sulfonic acid are e.g. alkali salts such as
sodium- or potassium salts, ammonium salts, morpholine salts, salts
of primary, sec. and tert. amines like monoethanolamine salts,
diethanolamine salts and the like; salicylate derivatives such as
isopropylbenzyl salicylate, benzyl salicylate, butyl salicylate,
ethylhexyl salicylate (PARSOL.RTM. EHS, Neo Heliopan OS), isooctyl
salicylate or homomethyl salicylate (homosalate, PARSOL.RTM. HMS,
Neo Heliopan HMS) and the like; triazine derivatives such as
ethylhexyl triazone (Uvinul T-150), diethylhexyl butamido triazone
(Uvasorb HEB) and the like. Encapsulated UV-filters such as
encapsulated ethylhexyl methoxycinnamate (Eusolex UV-pearls) or
microcapsules loaded with UV-filters as e.g. disclosed in EP
1471995 and the like;
[0057] Examples of broad spectrum or UV A screening agents i.e.
substances having absorption maximums between about 320 nm and 400
nm may be organic or inorganic compounds. Organic broad spectrum or
UV A screening agents include e.g. dibenzoylmethane derivatives
such as 4-tert.-butyl-4'-methoxydibenzoyl-methane (PARSOL.RTM.
1789), dimethoxydibenzoylmethane, isopropyldibenzoylmethane and the
like; benzotriazole derivatives such as
2,2'-methylene-bis-(6-(2H-benzotriazole-2-yl)-4-(1,1,3,3,-tetramethylbuty-
l)-phenol (Tinosorb M) and the like; bis-ethylhexyloxyphenol
methoxyphenyl triazine (Tinosorb S) and the like;
phenylene-1,4-bis-benzimidazolsulfonic acids or salts such as
2,2-(1,4-phenylene)bis-(1H-benzimidazol-4,6-disulfonic acid)
(Neoheliopan AP); amino substituted hydroxybenzophenones such as
2-(4-Diethylamino-2-hydroxy-benzoyl)-benzoic acid hexylester
(Uvinul A plus) as described in the European Patent Publication EP
1046391; Ionic UV-A filters as described in the International
Patent Publication WO2005080341 A1; As dibenzoylmethane derivatives
have limited photostability it may be desirable to photostabilize
these UV-A screening agents. Thus, the term "conventional UV-A
screening agent" also refers to dibenzoylmethane derivatives such
as e.g. PARSOL.RTM. 1789 stabilized by, e.g. 3,3-Diphenylacrylate
derivatives as described in the European Patent Publications EP 0
514 491 B1 and EP 0 780 119 A1; Benzylidene camphor derivatives as
described in the U.S. Pat. No. 5,605,680; Organosiloxanes
containing benzmalonate groups as described in the European Patent
Publications EP 0358584 B1, EP 0538431 B1 and EP 0709080 A1.
[0058] A good overview of UV-A- and UV-B screening agents which can
be added to the compositions of the present invention can also be
found in DE-A 103 27 432. All UV-screening agents disclosed in this
document are also useful as components for the compositions of the
present invention and are included herein by reference.
Additionally the composition of the present invention may contain
UV-A and UV-B filters. Further examples of UV-filters or screening
agents are disclosed, e.g., in WO 04/000256, see especially pages
10-12 which are included herein by reference.
[0059] A safe and effective amount of the UV-screening agent is
used, typically from about 1 wt.-% to about 20 wt.-%, more
typically from about 2 wt.-% to about 10 wt.-% based on the total
weight of the composition.
[0060] Other suitable UV-screening agents which may be incorporated
into the cosmetic or pharmaceutical topical compositions of the
present invention are inorganic pigments such as microparticulated
metal oxides (e.g. PARSOL.RTM. TX). Examples of such compounds
include e.g. titanium dioxide having an average primary particle
size of from about 15 nm to about 100 nm, zinc oxide having an
average primary particle size of from about 15 nm to about 150 nm,
zirconium oxide having an average primary particle size of from
about 15 nm to about 150 nm, iron oxide having an average primary
particle size of from about 15 nm to about 500 nm, and mixtures
thereof. The metal oxide particles may also be coated by metal
oxides such as e.g. aluminum or zirconium oxides or by organic
coatings such as e.g. polyols, methicone, aluminum stearate, alkyl
silane. Such coatings are well known in the art. When used herein,
the inorganic sunscreens are present in the amount of from about
0.1 wt.-% to about 20 wt.-%, preferably from about 0.5 wt.-% to
about 10 wt.-%, more preferably from about 1 wt.-% to about 5 wt.-%
based on the total weight of the composition.
[0061] The fatty acids or a salt, ester or amide thereof with the
preferences and definitions as given above are known or belong to a
known class of compounds and as such can be prepared by known
methods or in analogy thereto.
[0062] In another embodiment the invention relates to the use of a
fatty acid or a salt, ester or amide with the definitions and
preferences as given above for boosting the cosmetic effects of
retinoids and/or tanning actives.
[0063] The efficacy of the compositions of the invention comprising
fatty acid or a salt, ester or amide with the definitions and
preferences as given above, optionally in combination with a
retinoid as well as the concept of a synergistic effect between a
retinoid and a fatty acid as defined above may be demonstrated in
an in vitro test system using human primary keratinocytes as
outlined below. The marker may be the enzyme Transglutaminase 1,
which is a well-known and common differentiation marker in human
epidermal cells. Epidermal keratinocytes are isolated from human
foreskin biopsies and cultured in keratinocyte serum free medium
(KSFM, GIBCO) in a growth chamber with 37.degree. C. and 5%
CO.sub.2. At the second passage, cells are transferred to 6 well
plates and allowed to reach approximately 50% surface
confluence.
[0064] The active ingredient(s) are solubilized in ethanol or
ethanol/tetrahydrofuran. Retinoic acid solutions are handled under
yellow light conditions only. When keratinocyte cultures reaches
the appropriate confluence, the KSFM medium is supplemented with
1.3 mM calcium, in order to induce keratinocyte differentiation and
thus also induce TG1 expression, and treatment is started by adding
either a retinoid such as retinoic acid or a fatty acid or a salt,
ester or amide with the definitions and preferences as given above
or both substances in combination. For every sample, medium and/or
treatment substances are changed twice daily. Seventy-two hours
after the beginning of the treatment, cells are harvested and the
RNA extracted. RNA is reverse transcribed into cDNA. Relative
quantification of TG1 mRNA transcript levels in control versus
treatment cultures are determined using multiplexed real time PCR
analysis.
[0065] The ability of the cosmetic or pharmaceutical compositions
of the present invention to reduce skin wrinkles may be assessed by
profilometric methods described in "Skin topography measurement by
interference fringe projection: a technical validation". (Lagarde J
M; Rouvrais C; Black D; Diridollou S; Gall Y, Skin research and
technology: official journal of International Society for
Bioengineering and the Skin (ISBS) [and] International Society for
Digital Imaging of Skin (ISDIS) [and] International Society for
Skin Imaging (ISSI) (2001 May), 7(2), 112-21 or "Direct and
non-direct measurement techniques for analysis of skin surface
topography". Fischer T W; Wigger-Alberti W; Elsner P., Skin
pharmacology and applied skin physiology (1999 January-April),
12(1-2), 1-11.
[0066] The ability of the compounds and compositions of the present
invention to stimulate or protect hair growth may be determined
with a mouse model described for example in WO 9817273. Instead of
using Cyclophosphamide (Neostar, Pharmacia) to damage hair follicle
Mitomycin, or Methotrexate can be used. It is also possible to
detect hair growth acceleration with newborn mice. They have a
synchronized hair cycle and approximately after 3 weeks all hair
follicles go into the telogen phase. Then the animals are treated
and it is evaluated how fast and to what extend the hair is growing
Similar tests using in vitro or in vivo setups can also be found in
J. Invest. Dermato. symposium proceedings 3rd Int. Meeting of Hair
Research Societies, 8/1, p. 39-45 (2003).
[0067] The following examples exemplify the invention, but they
should not be construed as limiting the invention.
EXAMPLE 1
[0068] An anti-aging formulation containing the ingredients
indicated below can be prepared in a manner known per se.
TABLE-US-00001 Example formulation number 1 Ingredients % (w/w)
Glyceryl Myristate 4.00 Cetyl Alcohol 2.00 Steareth-2 2.00
Steareth-21 2.00 Isopropyl Myristate 5.00 Tocopheryl Acetate 0.50
Ethylhexyl Methoxycinnamate 4.00 Ethylhexyl Salicylate 2.00 Butyl
Methoxydibenzoylmethane 1.00 Almond Oil 2.00 BHT 0.05
Phenoxyethanol &Methylparaben & 0.80 Ethylparaben
&Propylparaben & Butylparaben &Isopropylparaben
Disodium EDTA 0.10 D-Panthenol 0.30 Propylene Glycol 4.00
Polyacrylamide &C13-14 Isoparaffin &Laureth-7 0.50
9-hydroxy stearic acid 0.50 Retinol 15D (Caprylic/Capric
Triglyceride & 0.50 Retinol) Water Ad 100 Triethanolamine
q.s.
EXAMPLE 2
[0069] An anti-aging formulations containing the ingredients
indicated below can be prepared in a manner known per se.
TABLE-US-00002 Example formulation number 2 Ingredients % (w/w)
Glyceryl Myristate 4.00 Cetyl Alcohol 2.00 Steareth-2 2.00
Steareth-21 2.00 Isopropyl Myristate 5.00 Tocopheryl Acetate 0.50
Ethylhexyl Methoxycinnamate 4.00 Ethylhexyl Salicylate 2.00 Butyl
Methoxydibenzoylmethane 1.00 Almond Oil 2.00 BHT 0.05
Phenoxyethanol &Methylparaben & 0.80 Ethylparaben
&Propylparaben & Butylparaben &Isopropylparaben
Disodium EDTA 0.10 D-Panthenol 0.30 Propylene Glycol 4.00
Polyacrylamide &C13-14 Isoparaffin &Laureth-7 0.50 Water Ad
100 9-hydroxy-stearic acid 0.50 Retinol Acetate 2.8 MI 0.10
Triethanolamine q.s.
EXAMPLE 3
[0070] A facial treatment formulation containing the ingredients
indicated below can be prepared in a manner known per se
TABLE-US-00003 Formulation No. 3 Ingredients % (w/w) Glyceryl
Myristate 5.00 Cetyl Alcohol 2.00 Cetyl Phosphate 2.00 Isopropyl
Myristate 10.00 Tocopheryl Acetate 0.30 Almond Oil 2.00 BHT 0.05
Phenoxyethanol &Methylparaben & 0.60 Ethylparaben
&Propylparaben & Butylparaben &Isopropylparaben
Tromethamine 0.90 Water Ad. 100 D-Panthenol 0.20 Disodium EDTA 0.10
Propylene Glycol 4.00 Polyacrylamide &C13-14 Isoparaffin
&Laureth-7 2.00 9-hydroxy stearic acid 0.50 Retinol 15D
(Caprylic/Capric Triglyceride & 0.50 Retinol) Triethanolamine
q.s.
EXAMPLE 4
[0071] A facial treatment formulation containing the ingredients
indicated below can be prepared in a manner known per se
TABLE-US-00004 Formulation No. 4 Ingredients % (w/w) Glyceryl
Myristate 5.00 Cetyl Alcohol 2.00 Cetyl Phosphate 2.00 Isopropyl
Myristate 10.00 Tocopheryl Acetate 0.30 Almond Oil 2.00 BHT 0.05
Phenoxyethanol &Methylparaben & 0.60 Ethylparaben
&Propylparaben & Butylparaben &Isopropylparaben
Tromethamine 0.90 Water Ad. 100 D-Panthenol 0.20 Disodium EDTA 0.10
Propylene Glycol 4.00 Polyacrylamide &C13-14 Isoparaffin
&Laureth-7 2.00 9-hydroxy stearic acid 0.50 Retinol Acetate 2.8
MI 0.10 Triethanolamine q.s.
EXAMPLE 5
[0072] Hair loss sera containing the ingredients indicated below
can be prepared in a manner known per se
TABLE-US-00005 Formulation No 5 Ingredients % (w/w) Water Ad. 100
Ethanol 8.00 Isopropanol 4.00 Propylene Glycol 5.00 D-Panthenol
0.20 PEG-12 Dimethicone 0.20 PEG-40 Hydrogenated Castor Oil 4.00
Phytantriol 0.05 Vitamin E Acetate 0.10 9-hydroxy stearic acid 0.50
Retinol 15D (Caprylic/Capric Triglyceride & 0.50 Retinol) NaOH
10% q.s.
EXAMPLE 6
[0073] Hair loss sera containing the ingredients indicated below
can be prepared in a manner known per se
TABLE-US-00006 Formulation No 6 Ingredients % (w/w) Water Ad. 100
Ethanol 8.00 Isopropanol 4.00 Propylene Glycol 5.00 D-Panthenol
0.20 PEG-12 Dimethicone 0.20 PEG-40 Hydrogenated Castor Oil 4.00
Phytantriol 0.05 Vitamin E Acetate 0.10 9-hydroxyy stearic acid
0.50 Retinol Acetate 2.8 MI 0.10 NaOH 10% q.s.
EXAMPLE 7
[0074] A skin fortifier lotion containing the ingredients indicated
below can be prepared in a manner known per se
TABLE-US-00007 Formulation No. 7 Ingredients % (w/w) Water Ad. 100
D-Panthenol 0.05 Sodium Ascorbyl Phosphate 0.20 Propylene Glycol
5.00 Acrylates/C10-30 Alkyl Acrylate Crosspolymer 0.50 Sodium
Hydroxide 30% 0.40 Disodium EDTA 0.10 Squalane 2.00 Phenoxyethanol
&Methylparaben & 0.80 Ethylparaben &Propylparaben &
Butylparaben &Isopropylparaben Coco-Caprylate/Caprate 4.00 BHT
0.05 Tocopheryl Acetate 0.10 Cyclomethicone 3.00 Glycerin 3.00
9-hydroxy stearic acid 0.50 Retinol 15D (Caprylic/Capric
Triglyceride & 0.50 Retinol) Sodium Hydroxide 10% q.s.
EXAMPLE 8
[0075] A skin fortifier lotion containing the ingredients indicated
below can be prepared in a manner known per se
TABLE-US-00008 Formulation No. 8 Ingredients % (w/w) Water Ad. 100
D-Panthenol 0.05 Sodium Ascorbyl Phosphate 0.20 Propylene Glycol
5.00 Acrylates/C10-30 Alkyl Acrylate Crosspolymer 0.50 Sodium
Hydroxide 30% 0.40 Disodium EDTA 0.10 Squalane 2.00 Phenoxyethanol
&Methylparaben & 0.80 Ethylparaben &Propylparaben &
Butylparaben &Isopropylparaben Coco-Caprylate/Caprate 4.00 BHT
0.05 Tocopheryl Acetate 0.10 Cyclomethicone 3.00 Glycerin 3.00
9-hydroxy stearic acid 0.50 Retinol Acetate 2.8 MI 0.10 Sodium
Hydroxide 10% q.s.
EXAMPLE 9
[0076] A formulation to treat age spots containing the ingredients
indicated below can be prepared in a manner known per se
TABLE-US-00009 Formulation No. 9 Ingredients % (w/w) Water Ad. 100
Polyquaternium-10 0.10 D-Panthenol 0.50 Sodium Ascorbyl Phosphate
1.00 Niacinamid 0.50 Propylene Glycol 4.00 Glycerin 3.00 PEG-12
Dimethicone 0.20 Disodium EDTA 0.10 Polysorbate 20 5.00
Phenoxyethanol &Methylparaben & 0.80 Ethylparaben
&Propylparaben & Butylparaben &Isopropylparaben
9-hydroxy stearic acid 0.50 Retinol 15D (Caprylic/Capric
Triglyceride & 0.50 Retinol) Sodium Hydroxide 10% q.s.
EXAMPLE 10
[0077] A formulation to treat age spots containing the ingredients
indicated below can be prepared in a manner known per se
TABLE-US-00010 Formulation No. 10 Ingredients % (w/w) Water Ad.
100. Polyquaternium-10 0.10 D-Panthenol 0.50 Sodium Ascorbyl
Phosphate 1.00 Niacinamid 0.50 Propylene Glycol 4.00 Glycerin 3.00
PEG-12 Dimethicone 0.20 Disodium EDTA 0.10 Polysorbate 20 5.00
Phenoxyethanol &Methylparaben & 0.80 Ethylparaben
&Propylparaben & Butylparaben &Isopropylparaben
9-hydroxy stearic acid 0.50 Retinol Acetate 2.8 MI 0.10 Sodium
Hydroxide 10% q.s.
EXAMPLE 11
[0078] Anti-cellulite formulations containing the ingredients
indicated below can be prepared in a manner known per se
TABLE-US-00011 Formulation No. 11 Ingredients % (w/w) Water Ad. 100
Caffeine 1.00 D-Panthenol 0.50 Glycerin 4.00 Butylene Glycol 2.00
Acrylates/C10-30 Alkyl Acrylate Crosspolymer 0.20 Disodium EDETA
0.10 Arachidyl Alcohol &Behenyl Alcohol &Arachidyl 5.00
Glucoside Squalane 2.00 Mineral Oil 4.00 Phenoxyethanol
&Methylparaben & 0.80 Ethylparaben &Propylparaben &
Butylparaben &Isopropylparaben Isononyl Isononanoate 4.00 BHT
0.05 Cetyl Alcohol 2.00 Dimethicone 0.50 Tocopheryl Acetate 0.10
9-hydroxy stearic acid 0.50 Retinol 15D (Caprylic/Capric
Triglyceride & 0.50 Retinol) Triethanolamine q.s.
EXAMPLE 12
[0079] An anti-cellulite formulation containing the ingredients
indicated below can be prepared in a manner known per se
TABLE-US-00012 Formulation No. 12 Ingredients % (w/w) Water Ad. 100
Caffeine 1.00 D-Panthenol 0.50 Glycerin 4.00 Butylene Glycol 2.00
Acrylates/C10-30 Alkyl Acrylate Crosspolymer 0.20 Disodium EDETA
0.10 Arachidyl Alcohol &Behenyl Alcohol &Arachidyl 5.00
Glucoside Squalane 2.00 Mineral Oil 4.00 Phenoxyethanol
&Methylparaben & 0.80 Ethylparaben &Propylparaben &
Butylparaben &Isopropylparaben Isononyl Isononanoate 4.00 BHT
0.05 Cetyl Alcohol 2.00 Dimethicone 0.50 Tocopheryl Acetate 0.10
9-hydroxy stearic acid 0.50 Retinol Acetate 2.8 MI 0.10
Triethanolamine q.s.
EXAMPLE 13
[0080] A skin repair formulation containing the ingredients
indicated below can be prepared in a manner known per se
TABLE-US-00013 Formulation No. 13 Ingredients % (w/w)
Polyglyceryl-2 Dipolyhydroxystearate 4.00 Polyglyceryl-3
Diisostearate 2.00 Beeswax 2.00 Zinc Stearate 2.00 Caprylic/Capric
Triglyceride 3.00 Cetearyl Isononanoate 8.00 Dicaprylyl Ether 5.00
BHT 0.05 Phenoxyethanol &Methylparaben & 0.60 Ethylparaben
&Propylparaben & Butylparaben &Isopropylparaben Water
Ad. 100 D-Panthenol 0.20 Disodium EDTA 0.10 Propylene Glycol 4.00
9-hydroxy stearic acid 0.55 Retinol 15D (Caprylic/Capric
Triglyceride & 0.50 Retinol)
EXAMPLE 14
[0081] A skin repair formulation containing the ingredients
indicated below can be prepared in a manner known per se
TABLE-US-00014 Formulation No. 14 Ingredients % (w/w)
Polyglyceryl-2 Dipolyhydroxystearate 4.00 Polyglyceryl-3
Diisostearate 2.00 Beeswax 2.00 Zinc Stearate 2.00 Caprylic/Capric
Triglyceride 3.00 Cetearyl Isononanoate 8.00 Dicaprylyl Ether 5.00
BHT 0.05 Phenoxyethanol &Methylparaben & 0.60 Ethylparaben
&Propylparaben & Butylparaben &Isopropylparaben Water
Ad. 100 D-Panthenol 0.20 Disodium EDTA 0.10 Propylene Glycol 4.00
9-hydroxy stearic acid 0.50 Retinol Acetate 2.8 MI 0.10
* * * * *