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|Title:||Methods for treatment of sundamaged human skin with retinoids|
|Abstract:||Various effects of photoaging or sundamage of skin including impairment of differentiation of epidermal epithelial cells and loss of collagen fibers, abnormal changes in elastic fibers and deterioration of small blood vessels in the dermis of the skin are retarded by applying topically to the epidermis in a maintenance therapy program effective amounts of retinoids including retinoid derivatives and stereoisomers thereof such that epithelial growths are substantially reduced and prevented and the skin substantially regains and maintains its firmness, turgor and elasticity. Moreover, with persistent treatment dermal blood cells and vessels increase and the epidermis and dermis thicken, resulting in improved ability of the skin to sense, resist and recover from irritation or injury. Further, hyperpigmentation, lines and wrinkles due to aging are reduced and prevented. The treatment is particularly useful for human facial skin and preferably applied in amounts insufficient to cause excessive irritation.|
|Inventor(s):||Kligman; Albert M. (Harvey Cedars, NJ)|
1. A method for retarding and reversing the loss of collagen fibers, abnormal changes in elastic fibers, and deterioration of small blood vessels in sundamaged human skin, comprising
applying topically to the surface of the skin a composition comprising effective amounts of a retinoid in a nontoxic, dermatologically acceptable vehicle in a program of maintenance therapy, whereby the skin substantially regains and maintains its
firmness, turgor and elasticity during said therapy, said composition and amounts of retinoid therein being selected so as to provide a dose for application which is insufficient to cause excessive irritation.
2. A method according to claim 1 wherein said retinoid is selected from the group consisting of retinoic acids, retinoic acid derivatives and stereoisomers thereof.
3. A method according to claim 2 wherein said retinoic acid, retinoic acid derivatives is selected from the group consisting of 13-cis-retinoic acid, 13cis-retinoic acid derivatives and thereof.
4. A method according to claim 1 wherein said retinoid is selected from the group consisting of (E)-4-[4-methyl-6-(2,6,6-trimethyl-1-cyclohexen-1-yl)-] benzoic acid; 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)ethylnyl]-benzoi c acid; and (E)-4-[2-(5,6,7,8-tetrahydro-7-hydroxy-5,5,8,8-tetramethyl-2-naphthalenyl- 1-propenyl] benzyl alcohol.
5. A method according to claim 1 wherein said retinoid is selected from the group consisting of 13-cis-retinoic acid; (all-E)-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetra enoic acid ethyl ester; (all-E)-9-(4-methoxy2,3,6,-trimethylphenyl)-3,7-dimethyl-2,4,6,8,-nonatetr aenoic acid; N-ethyl-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl2,4,6,8-nonatetrae namide; (E,E)-9-(2,6-dichloro-4-methoxy-3-methylphenyl)-3,7-dimethyl-2,4,6,8-nonat etraenoic acid ethyl ester; 7,8-didehydroretinoic acid; (E,E)-4-[2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1-yl)-1,3-butadienyl]ben zoic acid; (all-E)-3,7-dimethyl-(3-thienyl)-2,4,6,8-nonatetraconic acid; (E,E,E)-3-methyl-7-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl) -2,4,6-octatrienoic acid; (E)-6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthalenecarboxyl ic acid; (E,E,E)-7-(2,3-dihydro-1,1,3,3-tetramethyl-1H-inden-5-yl)-3-methyl-2,4,6-o ctatrienoic acid; (E)-4-[2-(2,3-dihydro-1,1,3,3-tetramethyl-1H-inden-5-yl)-1-propenyl]benzoi c acid; TTNPB (E)-4-[2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl-1propenyl] benzoic acid; (E)-4-[2-(5,6,7,8-tetrahydro-3-methyl-5,5,8,8-tetramethyl-2-naphthalenyl)- 1-propenyl]benzoic acid; (E)-1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-6-(1-methyl-2phenylethenyl) naphthalene; 6-(1,2,3,4-tetrahydro-1,1,4,4-tetra-methyl-6-naphthyl)-2-naphthalene-carbo xylic acid; .[.(E)-6-[2-(4-(ethylsulfonyl)phenyl]-1-methylethenyl]-1,2,3,4-tetrahydro- 1,2,3,4-tetrahydronaphth-7-yl)-1-[4-tetrazol-5-yl)phenyl]-1-propene.]. .Iadd.(E)-2-(1,1,4,4-tetramethyl-1,2,3,4-tetrahydronaphth-7-yl)-1-(4-tetra zol-5-yl)phenyl)-1-propene.Iaddend..
6. A method according to claim 1 wherein said skin is human facial skin.
7. A method according to claim 2 wherein said skin is human facial skin.
8. A method according to claim 3 wherein said skin is human facial skin.
9. A method according to claim 1 wherein said vehicle is a cream ointment.
10. A method according to claim 1 wherein said vehicle is an emollient vehicle.
11. A method according to claim 1 wherein said retinoid is retinol.
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