Formulations and methods for skin care or hyaluronic acid synthesis
Cosmetic and pharmaceutical formulations comprising specific amino acid combinations are described herein. Such formulations strengthen and enhance skin epithelial cell barrier function, thereby reducing moisture loss from the skin and restoring skin's structural integrity, epithelial differentiation, intercellular adhesion, and intracellular signaling and/or promoting maintenance of these features. Formulations described here comprise a therapeutically effective amount of free amino acids or a peptide combination of amino acids and either a therapeutically effective amount of a plant extract for skin barrier repair or a therapeutically effective amount of a retinoid for improving skin moisture. Also provided are injectable formulations described here for treating a subject suffering from osteoarthritis or symptoms thereof. Methods for administering these formulations for cosmetic and/or therapeutic purposes and uses thereof for same are also described herein, including the use thereof in the preparation of medicaments.
1. A topical formulation, comprising:
(a) as free amino acids or a peptide combination of amino acids, a therapeutically effective amount of a combination consisting of:
alanine, glutamine, glycine, and serine, or salts thereof,
wherein each free amino acid has a ratio to each of the other free amino acids of 1:100 or greater; and
(b) a therapeutically effective amount of a retinoid,
wherein the therapeutically effective amount of the combination and the therapeutically effective amount of the retinoid improve skin moisture when tested by a method detecting expression of epidermal growth factor (EGF) or hyaluronic acid (HA) marker gene and determining that the EGF marker gene expression or the HA marker gene expression is upregulated by 1.4 fold-450 fold for formulation treated skin cells as compared to untreated skin cells,
wherein the therapeutically effective amount of the combination and the therapeutically effective amount of the retinoid improves skin moisture; and
wherein the only amino acids present in the topical formulation are alanine, glutamine, glycine, and serine, or salts thereof.
2. The topical formulation according to claim 1 , wherein each of the amino acids is present at a concentration of: 0.1 mM or greater; 10 mM or less; or 0.1 mM to 10 mM.
3. The formulation according to claim 1 , wherein each of the amino acids is present at a weight percent to the formulation (wt/wt %) of 0.001 wt % or greater; 1 wt % or less; or 0.001 wt % to 1 wt %.
4. The topical formulation according to claim 1 , wherein the therapeutically effective amount of the retinoid is present at a weight percentage (w/w %) of the formulation of 0.01 w/w % or greater; 5 w/w % or less; or 0.01 w/w %-5 w/w %.
5. The topical formulation according to claim 1 , wherein the retinoid is selected from the group consisting of: retinyl; retinol or vitamin A; retinaldehyde or retinal; retinoic acid; or combinations thereof.
6. The topical formulation according to claim 1 , wherein the therapeutically effective amount of the combination of (a) and the therapeutically effective amount of the retinoid of (b) increase skin moisture, decrease loss of moisture, increase hyaluronic acid (HA), increase hyaluronic acid synthase (HAS), or combinations thereof.
7. The topical formulation according to claim 6 , wherein increasing HAS comprises increasing: HAS1 in fibroblasts, increasing HAS2 and/or HAS3 in keratinocytes, or combinations thereof.
8. The topical formulation according to claim 1 , further comprising:
a texturing and/or a bulking agent;
a phospholipid;
an anti-caking agent;
a dermatologically acceptable vehicle and/or additive; or
combinations thereof.
9. The topical formulation of claim 8 , wherein the bulking agent comprises cellulose, microcrystalline cellulose, or combinations thereof.
10. The topical formulation of claim 8 , wherein the phospholipid comprises lecithin, phosphatidylcholine, or combinations thereof.
11. The topical formulation of claim 8 , wherein the anti-caking agent comprises silica.
12. The topical formulation of claim 8 , wherein the additives are selected from the group consisting of: vitamins, minerals, preservatives, desquamation agents, anti-acne agents, anti-wrinkle agents/anti-atrophy agents, hydroxyl acids, anti-oxidants/radical scavengers, chelators, flavonoids, anti-inflammatory agents, anti-cellulite agents, topical anesthetics, tanning agents, skin lightening agents, skin soothing and skin healing agents, antimicrobial and antifungal agents, sunscreen agents, conditioning agents, structuring agents, thickening agent, and preservatives, or any combinations thereof.
13. The topical formulation according to claim 1 , wherein at least one amino acid is in L-form.
14. A method, comprising:
administering the topical formulation according to claim 1 to skin a subject suffering from a skin condition,
wherein, the method:
improves skin moisture;
increases HAS1 expression in fibroblasts;
increases HAS2 expression and/or HAS3 expression in keratinocytes; or combinations thereof.
15. The method according to claim 14 ,
wherein administering the topical formulation improves at least one visual property, or at least one tactile property, or a combination of visual and tactile properties of the skin,
wherein the skin condition comprises a cosmetic skin condition, atopic dermatitis, dermatitis, psoriasis, pruritus, eczema, a wound, or a burn.