Composition for enhancing lipid production, barrier function, hydrogen peroxide neutralization, and moisturization of the skin

A topical composition for enhancing the production of epidermal lipids, resulting from an admixture comprising:

• 0.001 to 40 wt % based on the weight of the composition of one or more derivatives or metabolites of L-leucine, L-isoleucine, and L-valine and mixtures thereof, which derivatives or metabolites are selected from the group consisting of:
• nor-leucine, nor-valine, L-alloisoleucine, L-threo-isoleucine, D, L, or DL-leucine-containing di- and tri-peptides, D, L or DL- valine-containing di- and tri-peptides, D, L or DL-isoleucine-containing di- and tri-peptides, nitrogen-free analogues of L-leucine, L-isoleucine and L-valine, branched chain keto acids derived from L-leucine, L-isoleucine, and L-valine, isovaleryl-CoA, isovalerylcarnitine, isovalerylglycine, isovaleric acid, beta-methylcrotonyl-CoA, beta-methylcrotonylcarnitine, beta-methylcrotonylglycine, beta-methylcrotonic acid, beta-methylglutaconyl-CoA, beta-methylglutaconylcarnitine, beta-methylglutaconylglycine, beta-methylglutaconic acid, beta-hydroxy-beta-methylglutaryl-CoA, beta-hydroxy-beta-methylglutarylcarnitine, beta-hydroxy-beta-methylglutarylglycine, beta-hydroxy-beta-methylglutaric acid, acetyl-CoA, acetylcarnitine, acetylglycine, acetoacetyl-CoA, acetoacetylcarnitine, acetoacetylglycine, isobutyryl-CoA, isobutyrylcarnitine, isobutyrylglycine, isobutyric acid, methylacrylyl-CoA, methylacrylylcarnitine, methylacrylylglycine, methylacrylic acid, beta-hydroxyisobutyryl-CoA, beta-hydroxyisobutyrylcarnitine, beta-hydroxyisobutyrylglycine, beta-hydroxyisobutyric acid, methylmalonate semialdehyde, propionyl-CoA, propionylcarnitine, propionylglycine, propionic acid, D-methylmalonyl-CoA, L-methylmalonyl-CoA, DL-methylmalonyl-CoA, D-methylmalonylcarnitine, L-methylmalonylcarnitine, DL-methylmalonylcarnitine, D-methylmalonylglycine, L-methylmalonylglycine, DL-methylmalonylglycine, methylmalonic acid, succinyl-CoA, succinylcarnitine, succinylglycine, succinic acid, alpha-methylbutyryl-CoA, alpha-methylbutyrylcarnitine, alpha-methylbutyrylglycine, alpha-methylbutyric acid, tiglyl-CoA, tiglylcarnitine, tiglylglycine, tiglic acid, alpha-methyl-beta-hydroxybutyryl-CoA, alpha-methyl-beta-hydroxybutyrylcarnitine, alpha-methyl-beta-hydroxybutyrylglycine, alpha-methyl-beta-hydroxybutyric acid, alpha-methylacetoacetyl-CoA, alpha-methylacetoacetylcarnitine, alpha-methylacetoacetylglycine, alpha-methylacetoacetic acid, and mixtures thereof;
• 0.001 to 20 wt %, based on the weight of the composition of one or more enzyme activators selected from the group consisting of octanoic acid, hexanoic acid, alpha keto isocaproic acid, alpha chloroisocaproic acid, thiamin diphosphate, and derivatives thereof, which one or more enzyme activators increase the rate of catabolism of the one or more derivatives or metabolites:
• a pharmaceutically acceptable or cosmetically acceptable carrier;
• and
• a container for containing the composition prior to application to the skin.

A method of enhancing the production of epidermal lipids, comprising:

• topically applying an effective amount of a topical composition which comprises
• 0.001 to 40 wt % based on the weight of the composition of one or more components selected from the group consisting of L-leucine, L-isoleucine, and L-valine, derivatives of L-leucine, L-isoleucine, and L-valine and mixtures thereof, which one or more components are capable of being catabolized in epidermal cells to form pro-lipids for epidermal lipid synthesis, and
• 0.001 to 20 wt %, based on the weight of the composition of one or more enzyme activators selected from the group consisting of octanoic acid, hexanoic acid. alpha keto isocaproic acid, alpha chloroisocaproic acid, thiamin diphosphate, and derivatives thereof, which one or more enzyme activators increase the rate of catabolism of the one or more components;
• to mammalian skin in an amount and for a period of time sufficient to enhance the production of epidermal lipids.

A method of increasing the cellular level of the natural moisturizing factor in the stratum corneum, comprising:

• topically applying an effective amount of a topical composition which comprises:
• 0.001 to 40 wt % based on the weight of the composition of one or more components selected from the group consisting of L-leucine, L-isoleucine, and L-valine, derivatives of L-leucine, L-isoleucine, and L-valine and mixtures thereof, which one or more components are capable of being catabolized in epidermal cells to produce metabolites and other amino acids, and
• 0.001 to 20 wt %, based on the weight of the composition of one or more enzyme activators selected from the group consisting of octanoic acid, hexanoic acid, alpha keto isocaproic acid, alpha chloroisocaproic acid, thiamin diphosphate, and derivatives thereof, which one or more enzyme activators increase the rate of catabolism of the one or more components
• to mammalian skin in an amount and for a period of time sufficient to increase the cellular level of natural moisturizing factor in the stratum corneum.

A method for increasing the production of vitamin D in the skin, comprising:

• topically applying an effective amount of a topical composition which comprises
• 0.001 to 40 wt % based on the weight of the composition of one or more components selected from the group consisting of L-leucine, L-isoleucine, and L-valine, derivatives of L-leucine. L-isoleucine, and L-valine and mixtures thereof, which one or more components are capable of being catabolized in epidermal cells to increase the production of cholesterol and other sterols in the skin, and
• 0.001 to 20 wt % based on the weight of the composition of one or more enzyme activators selected from the group consisting of octanoic acid, hexanoic acid, alpha keto isocaproic acid, alpha chloroisocaproic acid, thiamin diphosphate, and derivatives thereof, which one or more enzyme activators increase the rate of catabolism of the one or more components, wherein the one or more components selected from the group consisting of L-leucine, L-isoleucine, and L-valine, derivatives of L-leucine, L-isoleucine, and L-valine and mixtures thereof, and the enzyme activators are present in an amount and for a period of time sufficient to increase the production of cholesterol and other sterols in the skin;
• and
• exposing the skin to sunlight for a period of time sufficient to increase the production of vitamin D.

A method of neutralizing and detoxifying hydrogen peroxide by increasing the intra-cellular level of branched chain keto acids derived from L-leucine, L-isoleucine, and L-valine, comprising:

• topically applying an effective amount of a topical composition which comprises
• 0.001 to 40 wt % based on the weight of the composition of one or more components selected from the group consisting of L-leucine, L-isoleucine, and L-valine, derivatives of L-leucine, L-isoleucine, and L-valine and mixtures thereof, which one or more components are capable of being catabolized in epidermal cells to produce branched-chain keto acids derived from L-leucine, L-isoleucine, and L-valine and
• 0.001 to 25 wt % based on the weight of the composition of vitamin E;
• to the skin of an individual in an amount and for a period of time sufficient to increase the intra-cellular level of branched chain keto acids derived from L-leucine, L-isoleucine, and L-valine to neutralize and detoxify hydrogen peroxide.