WO1995024884A1 - Inhibition of hair growth - Google Patents
Inhibition of hair growth Download PDFInfo
- Publication number
- WO1995024884A1 WO1995024884A1 PCT/US1995/002898 US9502898W WO9524884A1 WO 1995024884 A1 WO1995024884 A1 WO 1995024884A1 US 9502898 W US9502898 W US 9502898W WO 9524884 A1 WO9524884 A1 WO 9524884A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- inhibitor
- hair growth
- arginine
- composition
- nitric oxide
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
- A61Q7/02—Preparations for inhibiting or slowing hair growth
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
- A61K2800/782—Enzyme inhibitors; Enzyme antagonists
Definitions
- the invention relates to a method of reducing unwanted hair growth in mammals.
- a main function of mammalian hair is to provide environmental protection. However, that function has largely been lost in humans, in whom hair is kept or removed from various parts of the body essentially for cosmetic reasons. For example, it is generally preferred to have hair on the scalp but not on the face.
- Various procedures have been employed to remove unwanted hair, including shaving, electrolysis, depilatory creams or lotions, waxing, plucking, and other cosmetic procedures, and therapeutic antiandrogens. These conventional procedures generally have drawbacks associated with them. Shaving, for instance, can cause nicks and cuts, and can leave a perception of an increase in the rate of hair regrowth. Shaving also can leave an undesirable stubble.
- Electrolysis can keep a treated area free of hair for prolonged periods of time, but can be expensive and painful, and it sometimes causes scarring.
- Depilatory creams though effective, typically are not recommended for frequent use due to their high irritancy potential. Waxing and plucking can cause pain, discomfort, in-grown hairs, and poor removal of short hair.
- antiandrogens -- which have been used to treat female hirsutism -- can have unwanted side effects.
- the rate and character of hair growth can be altered by applying to the skin inhibitors of certain enzymes.
- These inhibitors include inhibitors of 5-alpha reductase, ornithine decarboxylase, S-adenosylmethionine decarboxylase, gamma-glutamyl transpeptidase, and transglutaminase. See, - for example, Breuer et al., U.S. Pat. No. 4,885,289; Shander, U.S. Pat. No. 4,720,489; .Ahluwalia, U.S. Pat. No. 5,095,007; Ahluwalia et al., U.S. Pat. No.
- Nitric oxide synthetase forms nitric oxide by oxidizing one of the two terminal guanido nitrogens in L-arginine.
- the nitric oxide formed by the action of this enzyme is implicated in diverse physiological functions, including smooth muscle relaxation, immune system regulation, and neurotransmission.
- unwanted mammalian (including human) hair growth can be inhibited by topical application of an inhibitor of nitric oxide synthetase to the skin.
- the unwanted hair growth which is reduced may be normal hair growth which is cosmetically reduced, or hair growth that results from an abnormal or diseased condition.
- Preferred inhibitors of nitric oxide synthetase include N -methyl-L-arginine, N - r* nitro-L-arginine, N -nitro-L-arginine methyl ester, ⁇ -nitro-L-arginine benzyl ester, N- acetyl-L-arginine, N -amino-L-arginine, N- benzoy1-L-arginineamide, N-benzoyl-L-arginine methyl ester, N-benzoyl-L-arginine ethyl ester, N -allyl-L-arginine, N ⁇ -cyclopropy1-L-arginine, N-iminoethyl-L-ornithine, L-homoarginine, L- argininamide, diphenyleneiodonium, iodonium- diphenyl, and di-2-thienyliodonium. Irreversible inhibitors
- the inhibitor of nitric acid synthetase preferably is incorporated in a topical composition or a cosmetic composition which includes a non-toxic dermatologically acceptable vehicle or carrier which is adapted to be spread upon the skin.
- suitable vehicles are acetone, alcohols, or a cream, lotion, or gel which can effectively deliver the active compound.
- a penetration enhancer may be added to the vehicle to further enhance the effectiveness of the formulation.
- the concentration of the nitric oxide synthetase inhibitor in the composition may be varied over a wide range up to a saturated solution, preferably from 0.1% to 30% by weight or even more; the reduction of hair growth increases as the amount of inhibitor applied increases per unit area of skin.
- the maximum amount effectively applied is limited only by the rate at which the inhibitor penetrates the skin. Generally, the effective amounts range from 100 to 3000 micrograms or more per square centimeter of skin.
- the composition should be topically applied to a selected area of the body from which it is desired to inhibit hair growth.
- the composition can be applied to the face, particularly to the beard area of the face, i.e., the cheek, neck, upper lip, and chin.
- the composition can also be applied to the legs, arms, torso or armpits.
- the composition is particularly suitable for inhibiting the growth of unwanted hair in women suffering from hirsutism or other conditions.
- the composition should be applied once or twice a day, or even more frequently, for at least three months to achieve a perceived reduction in hair growth. Reduction in hair growth is demonstrated when the frequency or hair removal is reduced, or the subject perceives less hair on the treated site, or quantitatively, when the weight of hair removed by shaving (i.e., hair mass) is reduced.
- flank organs of each of a group of hamsters are depilated by applying a thioglycolate based chemical depilatory (Surgex) .
- Surgex a thioglycolate based chemical depilatory
- compositions provide an inhibition in hair growth of at least about 35%, more preferably at least about 50%, and most preferably at least about 70%, when tested in the Golden Syrian hamster assay.
- Vehicle A Pure water (68%), ethanol (16%), propylene glycol (5%), dipropylene glycol (5%) benzyl alcohol (4%) and propylene carbonate (2%)
- Vehicle B Pure water (80%), ethanol (10%) and propylene glycol (10%)
- the following assay measures the activity of nitric oxide synthetase in hair follicles.
- the assay can be used to evaluate the effectiveness of nitric oxide synthetase inhibitors in reducing nitric oxide synthetase activity.
- Hair follicles from hamster flank organ were excised, and an enzyme extract was prepared in buffered sucrose solution, pH 7.4, using a sonicator device.
- the sonicated extracts were centrifuged at 12,000 x g, and the clarified supernatant was analyzed for nitric oxide synthetase activity.
- follicle supernatant were added to 150 ⁇ l of an assay mixture containing 100 mM tris buffer (pH 7.5), 50 ⁇ M cold arginine, 1 ⁇ Ci/ml [ 3 H] - arginine, 3 mM CaCl 2 , and 1 mM NADPH warmed to 37°C, and incubated for 30 minutes at 37°C.
- Formation of the radiolabelled citrulline a coproduct of nitric oxide synthetase action that can be used to provide a measure of the enzyme activity, was determined using an HPLC methodology capable of separating citrulline from arginine. More specifically, after termination of the enzyme reaction by heating at 95°C.
- reaction mixture was centrifuged at 12,000 x g for 2 min.
- a 100 ⁇ l aliquot of the clarified supernatant containing reaction products was injected onto a cation exchange column (10 ⁇ Partisil 10-SAX 25 cm x 4.6 mm), and then eluted with 0.02 M monobasic potassium phosphate buffer (pH 4.5) . Under these conditions the elution time of citrulline and arginine are 6 and 7 min, respectively.
- HPLC effluent was collected in 1.0 ml fractions and the amount of radiolabelled citrulline formed in the assay was determined by scintillation counting.
- the enzyme activity was linear with respect to hair follicle extract added (i.e., protein concentration), as well as the time of incubation.
- Inhibitors of nitric oxide synthetase were evaluated as follows. Inhibitors at a final concentration of 1.0 mM were preincubated with the hair follicle enzyme extract (the supernatant) . The enzyme activity following exposure to the inhibitor was assayed as described above. This assay will be referred to herein as the "hair follicle nitric oxide synthetase inhibition assay.” The results are provided in Table 2.
Abstract
Description
Claims
Priority Applications (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CA002184171A CA2184171C (en) | 1994-03-16 | 1995-03-10 | Inhibition of hair growth |
EP95912801A EP0754023B1 (en) | 1994-03-16 | 1995-03-10 | Inhibition of hair growth |
MX9603930A MX9603930A (en) | 1994-03-16 | 1995-03-10 | Inhibition of hair growth. |
AU19843/95A AU681776B2 (en) | 1994-03-16 | 1995-03-10 | Inhibition of hair growth |
DE69509891T DE69509891T2 (en) | 1994-03-16 | 1995-03-10 | INHIBITION OF HAIR GROWTH |
JP52407695A JP3957745B2 (en) | 1994-03-16 | 1995-03-10 | Hair growth inhibition |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US213,931 | 1994-03-16 | ||
US08/213,931 US5468476A (en) | 1994-03-16 | 1994-03-16 | Reduction of hair growth |
Publications (1)
Publication Number | Publication Date |
---|---|
WO1995024884A1 true WO1995024884A1 (en) | 1995-09-21 |
Family
ID=22797082
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US1995/002898 WO1995024884A1 (en) | 1994-03-16 | 1995-03-10 | Inhibition of hair growth |
Country Status (11)
Country | Link |
---|---|
US (1) | US5468476A (en) |
EP (1) | EP0754023B1 (en) |
JP (1) | JP3957745B2 (en) |
AT (1) | ATE180404T1 (en) |
AU (1) | AU681776B2 (en) |
CA (1) | CA2184171C (en) |
DE (1) | DE69509891T2 (en) |
ES (1) | ES2131822T3 (en) |
MX (1) | MX9603930A (en) |
WO (1) | WO1995024884A1 (en) |
ZA (1) | ZA952095B (en) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2730930A1 (en) * | 1995-02-27 | 1996-08-30 | Oreal | USE OF NO-SYNTHASE INHIBITORS TO REDUCE THE IRRITANT SKIN EFFECT OF PRODUCTS USED IN THE COSMETIC OR PHARMACEUTICAL FIELD |
WO1998036730A2 (en) * | 1997-02-21 | 1998-08-27 | Beiersdorf Ag | Compositions for treating acne rosacea |
US9655833B2 (en) | 2009-07-29 | 2017-05-23 | Elise OLSEN | Compositions and methods for inhibiting hair growth |
Families Citing this family (43)
Publication number | Priority date | Publication date | Assignee | Title |
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GB9200114D0 (en) * | 1992-01-04 | 1992-02-26 | Scras | Dual inhibitors of no synthase and cyclooxygenase |
US5648394A (en) * | 1993-05-27 | 1997-07-15 | Boxall; Brian Alfred | Topical composition for inhibiting hair growth |
US5728736A (en) * | 1995-11-29 | 1998-03-17 | Shander; Douglas | Reduction of hair growth |
US5652273A (en) | 1995-11-30 | 1997-07-29 | Henry; James | Reduction of hair growth |
US6407056B1 (en) | 1996-07-12 | 2002-06-18 | Johnson & Johnson Consumer Companies, Inc. | Methods for altering hair growth and hair pigmentation by apoptosis in the follicular papillae and compositions therefor |
WO1998048826A1 (en) * | 1997-04-30 | 1998-11-05 | Northwestern University | Inhibition of nitric oxide synthase by amino acids and dipeptides |
JP3973748B2 (en) * | 1998-01-14 | 2007-09-12 | 花王株式会社 | Hair growth inhibitor |
US6346519B1 (en) | 1998-09-09 | 2002-02-12 | Advanced Medical Instruments | Method and composition for treating arthritis |
US6808716B2 (en) | 1999-01-08 | 2004-10-26 | Ruey J. Yu | N-acetylamino acids, related N-acetyl compounds and their topical use |
US6159485A (en) | 1999-01-08 | 2000-12-12 | Yugenic Limited Partnership | N-acetyl aldosamines, n-acetylamino acids and related n-acetyl compounds and their topical use |
US6121269A (en) * | 1999-02-22 | 2000-09-19 | Henry; James P. | Reduction of hair growth |
FR2794974B1 (en) * | 1999-06-16 | 2001-08-17 | Exsymol Sa | COSMETIC COMPOSITION FOR SLIMMING BASED ON L-ARGININE, AN ANALOG OF L-ARGININE OR A DERIVATIVE THEREOF, APPLICABLE TOPICALLY |
US6573299B1 (en) | 1999-09-20 | 2003-06-03 | Advanced Medical Instruments | Method and compositions for treatment of the aging eye |
DE60022892T2 (en) * | 1999-10-21 | 2006-07-13 | Kao Corp. | Method of depilation |
US6235737B1 (en) | 2000-01-25 | 2001-05-22 | Peter Styczynski | Reduction of hair growth |
US6299865B1 (en) | 2000-05-02 | 2001-10-09 | Peter Styczynski | Reduction of hair growth |
FR2808525A1 (en) * | 2000-05-05 | 2001-11-09 | Sod Conseils Rech Applic | New amidino- or guanidino-substituted aminoacid derivatives, are nitrogen monoxide synthase inhibitors useful for treating cardiovascular, cerebrovascular or central or peripheral nervous system disorders |
EP1296943A1 (en) * | 2000-05-05 | 2003-04-02 | Societe De Conseils De Recherches Et D'applications Scientifiques S.A. (S.C.R.A.S.) | Amino acid derivatives and their use as medicines |
US7439271B2 (en) | 2001-06-27 | 2008-10-21 | The Gillette Company | Reduction of hair growth |
JP4759182B2 (en) * | 2001-08-03 | 2011-08-31 | 花王株式会社 | Water-soluble ginger extract |
US6743822B2 (en) | 2001-08-10 | 2004-06-01 | The Gillette Company | Reduction of hair growth |
US7261878B2 (en) * | 2001-08-10 | 2007-08-28 | The Gillette Company | Reduction of hair growth |
US20030036561A1 (en) * | 2001-08-10 | 2003-02-20 | Peter Styczynski | Reduction of hair growth |
AUPR988202A0 (en) * | 2002-01-09 | 2002-01-31 | University Of Adelaide, The | Animal husbandry hair removal method |
US20040198821A1 (en) * | 2002-01-29 | 2004-10-07 | Hwang Cheng Shine | Reduction of hair growth |
US7160921B2 (en) * | 2002-01-29 | 2007-01-09 | The Gillette Company | Reduction of hair growth |
US20030199584A1 (en) * | 2002-04-11 | 2003-10-23 | Ahluwalia Gurpreet S. | Reduction of hair growth |
US20040077593A1 (en) * | 2002-10-21 | 2004-04-22 | Marron Susan M. | Numbing gel for hair removal |
US20040141935A1 (en) * | 2003-01-21 | 2004-07-22 | Peter Styczynski | Reduction of hair growth |
US7015349B2 (en) * | 2003-03-26 | 2006-03-21 | The Gillette Company | Reduction of hair growth |
US20050031699A1 (en) * | 2003-06-26 | 2005-02-10 | L'oreal | Porous particles loaded with cosmetically or pharmaceutically active compounds |
EP1750736B1 (en) * | 2004-01-16 | 2010-04-21 | Cognis France, S.A.S. | Uses for the extract of gymnema sylvestris |
US20050249685A1 (en) * | 2004-04-27 | 2005-11-10 | Natalia Botchkareva | Reduction of hair growth |
KR20070086431A (en) * | 2004-12-22 | 2007-08-27 | 더 지렛트 캄파니 | Reduction of hair growth with survivin inhibitors |
MX2007007623A (en) * | 2004-12-22 | 2007-08-03 | Gillette Co | Reduction of hair growth. |
US20060263438A1 (en) * | 2005-05-17 | 2006-11-23 | L'oreal | Gelled oil particles for targeting sebaceous glands and/or hair follicles |
EP1726292A1 (en) * | 2005-05-23 | 2006-11-29 | Reckitt Benckiser (UK) LIMITED | Composition comprising resveratrol and topical use thereof for reducing human hair growth |
US7618956B2 (en) * | 2005-05-31 | 2009-11-17 | The Gillette Company | Reduction of hair growth |
US20070059264A1 (en) * | 2005-09-13 | 2007-03-15 | Ahluwalia Gurpreet S | Reduction of hair growth |
US7727516B2 (en) * | 2006-02-28 | 2010-06-01 | The Procter & Gamble Company | Reduction of hair growth |
US7282225B1 (en) | 2006-09-27 | 2007-10-16 | Occular Technologies, Inc. | Composition and methods for improving retinal health |
FR2944443B1 (en) | 2009-04-21 | 2012-11-09 | Arkema France | METHOD FOR MANUFACTURING IMPREGNATED FREE POLYAMIDE FREE POWDER PARTICLES, AND POLYAMIDE FREE POWDER PARTICLES HAVING A CONTENT OF AT LEAST 25% BY WEIGHT OF AT LEAST ONE COSMETIC OR PHARMACEUTICAL AGENT |
FR2953716B1 (en) | 2009-12-16 | 2015-03-27 | Oreal | KIT FOR FORMULATING A COSMETIC PRODUCT |
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Publication number | Priority date | Publication date | Assignee | Title |
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WO1986002269A1 (en) * | 1984-10-15 | 1986-04-24 | Handelman, Joseph, H. | Hair growth modification |
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US4161540A (en) * | 1966-08-22 | 1979-07-17 | Schering Corporation | Antiandrogenic agents and methods for the treatment of androgen dependent disease states |
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US4039669A (en) * | 1975-08-01 | 1977-08-02 | Sterling Drug Inc. | Composition for topical application and use thereof |
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US5095007A (en) * | 1990-10-24 | 1992-03-10 | Ahluwalia Gurpreet S | Alteration of rate and character of hair growth |
DE4038693A1 (en) * | 1990-12-05 | 1992-06-11 | Heverhagen Ulrich | MEANS TO REDUCE GROWTH OR TO REMOVE HAIR ON HUMAN BODY |
US5143925A (en) * | 1990-12-20 | 1992-09-01 | Douglas Shander | Alteration of rate and character of hair growth |
GB9118866D0 (en) * | 1991-09-04 | 1991-10-23 | Unilever Plc | Cosmetic composition |
-
1994
- 1994-03-16 US US08/213,931 patent/US5468476A/en not_active Expired - Lifetime
-
1995
- 1995-03-10 WO PCT/US1995/002898 patent/WO1995024884A1/en active IP Right Grant
- 1995-03-10 AU AU19843/95A patent/AU681776B2/en not_active Ceased
- 1995-03-10 MX MX9603930A patent/MX9603930A/en unknown
- 1995-03-10 AT AT95912801T patent/ATE180404T1/en not_active IP Right Cessation
- 1995-03-10 ES ES95912801T patent/ES2131822T3/en not_active Expired - Lifetime
- 1995-03-10 CA CA002184171A patent/CA2184171C/en not_active Expired - Fee Related
- 1995-03-10 EP EP95912801A patent/EP0754023B1/en not_active Expired - Lifetime
- 1995-03-10 DE DE69509891T patent/DE69509891T2/en not_active Expired - Lifetime
- 1995-03-10 JP JP52407695A patent/JP3957745B2/en not_active Expired - Fee Related
- 1995-03-14 ZA ZA952095A patent/ZA952095B/en unknown
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1986002269A1 (en) * | 1984-10-15 | 1986-04-24 | Handelman, Joseph, H. | Hair growth modification |
Cited By (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2730930A1 (en) * | 1995-02-27 | 1996-08-30 | Oreal | USE OF NO-SYNTHASE INHIBITORS TO REDUCE THE IRRITANT SKIN EFFECT OF PRODUCTS USED IN THE COSMETIC OR PHARMACEUTICAL FIELD |
WO1996026711A1 (en) * | 1995-02-27 | 1996-09-06 | L'oreal | Nitric oxide synthase inhibitors |
US7083799B1 (en) | 1995-02-27 | 2006-08-01 | L'oreal | No-synthase inhibitors |
WO1998036730A2 (en) * | 1997-02-21 | 1998-08-27 | Beiersdorf Ag | Compositions for treating acne rosacea |
WO1998036730A3 (en) * | 1997-02-21 | 1998-10-22 | Beiersdorf Ag | Compositions for treating acne rosacea |
US9655833B2 (en) | 2009-07-29 | 2017-05-23 | Elise OLSEN | Compositions and methods for inhibiting hair growth |
US9707169B2 (en) | 2009-07-29 | 2017-07-18 | Elise OLSEN | Compositions and methods for inhibiting hair growth |
US10159634B2 (en) | 2009-07-29 | 2018-12-25 | Elise A. Olsen | Compositions and methods for inhibiting hair growth |
EP3871671A2 (en) | 2009-07-29 | 2021-09-01 | Olsen, Elise | Fp receptor antagonists for inhibiting hair growth |
Also Published As
Publication number | Publication date |
---|---|
EP0754023B1 (en) | 1999-05-26 |
CA2184171C (en) | 1999-08-10 |
AU1984395A (en) | 1995-10-03 |
EP0754023A1 (en) | 1997-01-22 |
JP3957745B2 (en) | 2007-08-15 |
ZA952095B (en) | 1995-12-11 |
AU681776B2 (en) | 1997-09-04 |
ES2131822T3 (en) | 1999-08-01 |
MX9603930A (en) | 1997-04-30 |
US5468476A (en) | 1995-11-21 |
CA2184171A1 (en) | 1995-09-21 |
JPH09510447A (en) | 1997-10-21 |
DE69509891D1 (en) | 1999-07-01 |
ATE180404T1 (en) | 1999-06-15 |
DE69509891T2 (en) | 1999-12-09 |
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