Topical benfotiamine and pyridoxamine compositions

Abstract

The present invention provides a composition comprising an effective amount of benfotiamine and an effective amount of pyridoxamine in a suitable vehicle for topical application. The present compositions are useful in improving the appearance of aged skin characterized by wrinkles, loss of elasticity, and hyperpigmentation caused by chronoaging and/or photoaging of skin, by inhibiting particularly skin damage resulting from reactive carbonyl species (RCS), glycation of skin proteins, formation of advanced glycation endproducts (AGEs) and formation of advanced lipoxidation endproducts (ALEs).

What is claimed is: 
     
         1 . A topical composition comprising:
 (i) a benfotiamine or a dermatologically acceptable salt thereof;   (ii) a pyridoxamine or a dermatologically acceptable salt thereof; and   (iii) a dermatologically acceptable carrier;   the pyridoxamine and benfotiamine components being incorporated in amounts effective in the treatment of skin damage.   
     
     
         2 . The composition of  claim 1 , which comprises component (i) in an amount of from about 0.001 to 80% by weight, based on the total weight of the composition. 
     
     
         3 . The composition of  claim 1 , which comprises component (ii) in an amount of from about 0.001 to 80% by weight, based on the total weight of the composition. 
     
     
         4 . The composition of  claim 1 , further comprising an antioxidant. 
     
     
         5 . The composition of  claim 4 , wherein the antioxidant is selected from the group consisting of grape seed procyanidins, tocopherols, tocotrienols, astaxanthin, carnosol or carnosic acid, macqui berry anthocyanins, billberry anthocyanins, blueberry anthocyanins, pomegranate extract, ellagic acid, honokiol, magnolol, silymarin, quercetin, naringenin, rosmarinic acid, clove essential oil, emblica extract, thiotaurine, acai extract, aronia extract, mangosteen and  camellia sinensis  extract. 
     
     
         6 . The composition of  claim 4 , wherein the antioxidant is an endogenous antioxidant or antioxidant enzyme selected from the group consisting of a superoxide dismutase, glutathione, reduced glutathione, glutathione peroxidase, glutathione s-transferase, glutathione reductase, thioredoxin, NADH/NADPH, r-lipoic acid, R-dihydrolipoic acid, and catalase. 
     
     
         7 . The composition of  claim 1 , further comprising an additional AGE inhibitor. 
     
     
         8 . The composition of  claim 6 , wherein the additional AGE inhibitor is selected from the group consisting of carnosine, a carnosine derivate, a carnosine salt, a thiamine or a coenzymated thiamine, thiamine pyrophosphate, pyridoxamine-5-phosphate and pyridoxamine-5-phosphate. 
     
     
         9 . The composition of  claim 1 , further comprising an anthocyanin and a glutathione. 
     
     
         10 . The composition of  claim 1 , further comprising a hydroxylamine 
     
     
         11 . The composition of  claim 10  wherein that hydroxylamine is an anti-glycation agent and/or lipofuscin inhibitor. 
     
     
         12 . The composition of  claim 12  wherein the hydroxylamine is N-tert-butyl hydroxylamine. 
     
     
         13 . The composition of  claim 1 , further comprising a spintrap. 
     
     
         14 . The composition of  claim 1 , further comprising an acetyl-choline precursor or an acetylcholinesterase inhibitor. 
     
     
         15 . The composition of  claim 13  wherein the acetyl-choline precursor or acetylcholinesterase inhibitor is Huperzine-A or an extract containing Huperzine-A. 
     
     
         16 . The composition of  claim 1 , further comprising a dermorelaxant. 
     
     
         17 . The composition of  claim 1  further comprising centrophenoxine 
     
     
         18 . The composition of  claim 1  wherein the formulation contains only natural or nature-identical ingredients. 
     
     
         19 . The composition of  claim 18 , further comprising a botanical or plant-derived preservative. 
     
     
         20 . The composition of  claim 1 , further comprising a container, wherein the container is airtight, the container substantially blocks light between 450 and 720 nm, or a combination thereof. 
     
     
         21 . The composition of  claim 1  whereas the components are encapsulated in liposomes or nanosomes. 
     
     
         22 . The composition of  claim 1  further contains ascorbic acid or a derivative of ascorbic acid, wherein the ascorbic acid is stabilized by encapsulation with emblica tannins, NADH, r-DHLA, glutathione, anthocyanins, or a combination thereof. 
     
     
         23 . A method of inhibiting the formation of advanced glycation endproducts in the skin, said method comprising topically applying to skin areas to be treated a composition comprising:
 (i) a benfotiamine or a dermatologically acceptable salt thereof;   (ii) a pyridoxamine or a dermatologically acceptable salt thereof; and   (iii) a dermatologically acceptable carrier;   
       the pyridoxamine and benfotiamine components being incorporated in amounts effective in the inhibition of the formation of advanced glycation endproducts. 
     
     
         24 . The method of  claim 23 , wherein the composition further comprises an antioxidant. 
     
     
         25 . The method of  claim 24 , wherein the antioxidant is selected from the group consisting of grape seed procyanidins, tocopherols, tocotrienols, astaxanthin, carnosine or carnosic acid, macqui berry anthocyanins, billberry anthocyanins, blueberry anthocyanins, pomegranate extract, ellagic acid, honokiol, magnolol, silymarin, quercetin, naringenin, rosmarinic acid, clove essential oil, emblica extract, thiotaurine, acai extract, aronia extract, mangosteen and  camellia sinensis  extract. 
     
     
         26 . The method of  claim 23 , wherein the composition further comprises an additional AGE inhibitor, 
     
     
         27 . The method of  claim 23 , further comprising orally administering an AGE inhibitor. 
     
     
         28 . The method of  claim 23 , wherein inhibition of the formation of advanced glycation endproducts occurs after or concurrently with the oral ingestion or topical application of a sugar, amino acid, or vitamin C derivative, wherein the sugar, amino acid, or vitamin C derivative is either prone to glycation or has an oxidation product that is prone to glycation or is itself a glycating agent. 
     
     
         29 . The method of  claim 23 , wherein the composition further comprises a dermorelaxant, and wherein the skin areas to be treated are skin areas covering expression muscles. 
     
     
         30 . The method of  claim 23 , wherein the composition further comprises an ingredient having muscle toning properties wherein the skin areas to be treated are skin areas covering muscles known to sag and loose their tone due to the aging process. 
     
     
         31 . The method of  claim 23 , wherein the composition is applied in a makeup. 
     
     
         32 . The method of  claim 23 , wherein inhibiting the formation of advanced glycation endproducts comprises reducing the advanced glycation endproduct formation in the skin by at least 50%. 
     
     
         33 . The method of  claim 23 , further comprising inhibiting the formation of advanced lipoxidation end products.