Topical compositions and methods for epithelial-related conditions

Abstract

The present invention relates to pharmaceutical, cosmetic and cosmeceutical topical compositions containing polyisoprenyl-protein inhibitor compounds and methods useful in the promotion of healthy epithelium and the treatment of epithelial-related conditions

1 - 90 . (canceled) 
     
     
         91 . A topical composition comprising:
 at least one polyisoprenyl-protein inhibitor compound present in the amount of about 0.01% to about 50%, wherein the at least one polyisoprenyl-protein inhibitor compound comprises a compound of formula 1:   
       
         
           
           
               
               
           
         
       
       or pharmaceutically acceptable salts and esters thereof, 
       wherein R 1  is alkyl of 1 to 3 carbon atoms; 
       R 2  is —COX; wherein X is —OH, —OCH 3 , —NH 2 , —NHR 4 , —N(R 4 ) 2  or halogen; 
       R 3  is a straight or branched chain alkyl of 10 to 25 carbon atoms or a straight or branched chain alkenyl of 10 to 25 carbon atoms; 
       R 4  is an alkyl of 1 to 25 carbon atoms; and
 a carrier selected from the group consisting of: water, ethanol, isopropanol, acetone, and combinations thereof. 
 
     
     
         92 . The topical composition of  claim 91 , wherein R 1  is methyl, R 2  is COOH, and R 3  is farnesyl. 
     
     
         93 . The composition of  claim 91 , wherein R 1  is methyl, X is OCH 3 , and R 3  is farnesyl. 
     
     
         94 . The composition of  claim 91 , further comprising a retinoid selected from the group consisting of: vitamin A, retinol, retinal, retinyl palmitate, retinoic acid, tretinoin, iso-tretinoin, and combinations thereof. 
     
     
         95 . The composition of  claim 91 , further comprising an alpha-hydroxy acid selected from the group consisting of: glycolic acid, lactic acid, tartaric acid, malic acid, citric acid, and combinations thereof. 
     
     
         96 . The composition of  claim 91 , further comprising titanium oxide, zing oxide, benzoyl peroxide, fluorouracil, resorcinol, salicylic acid, or a mixture thereof. 
     
     
         97 . The composition of  claim 91 , wherein the topical formulation is in the form of a powder, an oil, a cream, a gel, or a bandage. 
     
     
         98 . The composition of  claim 91 , wherein the carrier is selected from the group consisting of: a moisturizing agent, a pH adjusting agent, a deodorant agent, a thickener, a solubilizing agent, a penetration enhancer, an anti-irritant, a colorant, a surfactant, and combinations thereof. 
     
     
         99 . The composition of  claim 91 , further comprising an active ingredient selected from the group consisting of: a protective agent, an emollient, an astringent, an irritant, a keratolytic agent, a sun screening agent, a sun tanning agent, an antibiotic agent, an antifungal agent, an antiviral agent, an antiprotozoal agent, an anti-acne agent, an anesthetic agent, a steroid anti-inflammatory agent, a non-steroidal anti-inflammatory agent, an antipruruitic agent, an ant-oxidant agent, a chemotherapeutic agent, an anti-histimine agent, a vitamin, a hormone, an anti-dandruff agent, an anti-wrinkle agent, an anti-skin atrophy agent, a sclerosing agent, a cleansing agent, a caustic agent, a hypo-pigmenting agent, and combinations thereof. 
     
     
         100 . A cosmetic composition for reducing inflammation in humans when applied to a skin surface of a human, the cosmetic composition comprising:
 at least one polyisoprenyl-protein inhibitor compound comprising a compound of formula 1:   
       
         
           
           
               
               
           
         
       
       or pharmaceutically acceptable salts and esters thereof, 
       wherein R 1  is alkyl of 1 to 3 carbon atoms; 
       R 2  is —COX; wherein X is —OH, —OCH 3 , —NH 2 , —NHR 4 , —N(R 4 ) 2  or halogen; 
       R 3  is a straight or branched chain alkyl of 10 to 25 carbon atoms or a straight or branched chain alkenyl of 10 to 25 carbon atoms; 
       R 4  is an alkyl of 1 to 25 carbon atoms; and
 a carrier selected from the group consisting of: water, ethanol, isopropanol, acetone, and combinations thereof. 
 
     
     
         101 . The cosmetic composition of  claim 100 , wherein the at least one polyisoprentyl-protein inhibitor is N-acetyl-5-farnesylcystein (“AFC”) and wherein the AFC is present in an amount of from about 0.01% to about 50% of the cosmetic composition. 
     
     
         102 . The cosmetic composition of  claim 100 , wherein the composition is in the form of a powder, an oil, a cream, a gel, or a bandage. 
     
     
         103 . The composition of  claim 101 , further comprising a retinoid selected from the group consisting of: vitamin A, retinol, retinal, retinol palmitate, retinoic acid, tretinoin, iso-tretinoin, and combinations thereof. 
     
     
         104 . The composition of  claim 101 , further comprising an alpha-hydroxy acid selected from the group consisting of: glycolic acid, lactic acid, tartaric acid, malic acid, citric acid, and combinations thereof. 
     
     
         105 . The composition of  claim 101 , further comprising titanium oxide, zing oxide, benzoyl peroxide, fluorouracil, resorcinol, salicylic acid, or mixtures thereof. 
     
     
         106 . The composition of  claim 101 , wherein the topical formulation is in the form of a powder, an oil, a cream, a gel, or a bandage. 
     
     
         107 . The composition of  claim 101 , wherein the carrier is selected from the group consisting of: a moisturizing agent, a pH adjusting agent, a deodorant agent, a thickener, a solubilizing agent, a penetration enhancer, an anti-irritant, a colorant, a surfactant, and combinations thereof. 
     
     
         108 . The composition of  claim 101 , further comprising an active ingredient selected from the group consisting of: a protective agent, an emollient, an astringent, an irritant, a keratolytic agent, a sun screening agent, a sun tanning agent, an antibiotic agent, an antifungal agent, an antiviral agent, an antiprotozoal agent, an anti-acne agent, an anesthetic agent, a steroid anti-inflammatory agent, a non-steroidal anti-inflammatory agent, an antipruruitic agent, an ant-oxidant agent, a chemotherapeutic agent, an anti-histimine agent, a vitamin, a hormone, an anti-dandruff agent, an anti-wrinkle agent, an anti-skin atrophy agent, a sclerosing agent, a cleansing agent, a caustic agent, a hypo-pigmenting agent, and combinations thereof. 
     
     
         109 . A method of promoting healthy skin in an individual, the method comprising: 
       topically applying to a surface of a human in need thereof, an effective amount of at least one polyisoprenyl-protein inhibitor compound present in an amount of from about 0.01% to about 50%, wherein the at least one polyisoprenyl-protein inhibitor compound comprises a compound of formula 1: 
       
         
           
           
               
               
           
         
       
       or pharmaceutically acceptable salts and esters thereof, 
       wherein R 1  is alkyl of 1 to 3 carbon atoms; 
       R 2  is —COX; wherein X is —OH, —OCH 3 , —NH 2 , —NHR 4 , —N(R 4 ) 2  or halogen; 
       R 3  is a straight or branched chain alkyl of 10 to 25 carbon atoms or a straight or branched chain alkenyl of 10 to 25 carbon atoms; 
       R 4  is an alkyl of 1 to 25 carbon atoms; and
 a carrier selected from the group consisting of: water, ethanol, isopropanol, acetone, and combinations thereof. 
 
     
     
         110 . The method of  claim 109 , wherein the at least one polyisoprentyl-protein inhibitor is N-acetyl-5-farnesylcystein (“AFC”).