Compositions for nail and skin treatment

Abstract

Novel topical compositions for the treatment of nail and skin afflictions comprising at least one active agent, at least one volatile solvent, at least one film-forming ingredient and at least one phospholipid, processes for their preparation and methods of treatment of nail and skin afflictions. Following application of the compositions and evaporation of volatile solvents, the composition produces a film, which has web-like structures containing the active agent(s).

1 . A topical composition for the treatment of nail or skin afflictions in a human or animal, comprising 0.01-20% of at least one active agent, 0.2-20% of a phospholipid, 50-90% of volatile solvents selected from ethyl acetate, C2-C4 alcohols or combinations thereof, 0-40% water, 0-30% of a glycol, 0.2-15% of a film-forming ingredient and optionally 0-5% other pharmaceutically acceptable ingredients, wherein following the rapid evaporation of the volatiles, a continuous film is formed on the nail or skin surface treated, said film exhibiting a web-like structure comprising the active agent(s). 
     
     
         2 . The composition of  claim 1 , wherein the said glycol is selected from ethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol, tetraglycol, butylene glycol, hexylene glycol and glycol esters or ethers like ethylene glycol monomethyl ether, diethylene glycol monoethyl ether, or other pharmaceutically acceptable glycols and combinations thereof. 
     
     
         3 . The composition of  claim 1 , wherein the at least one active agent is selected from antimicrobials, antivirals, anti-mycotics, anti-parasitics, anti-worms, anti-ringworms, anti-warts, anti-yeast, vasodilators, vasoconstrictors, vitamins, impetigo treatments, immuno suppressing agents, anti-psoriasis drugs, melanin, pigments, peptides, amino-acids, hormones, anti-cancer, analgesic, anesthetic, antihistamines, steroids, retinoids, anti-acne drugs, atopic dermatitis drugs, rosacea drugs, keratosis pilaris drugs, dermatitis drugs, anti-eczema drugs, anti-hyperhidrosis drugs, skin discoloration drugs and combinations thereof. 
     
     
         4 . The composition of  claim 1 , wherein the at least one active agent is selected from ciclopirox, amorolfine, griseofulvine, posaconazole, itraconazole, econazole, ibuprofen, butenafine, borax, geraniol, erbinafine and salts thereof, and combinations thereof. 
     
     
         5 - 6 . (canceled) 
     
     
         7 . The composition of  claim 1 , wherein the phospholipid is selected from soy lecithin, egg lecithin, phosphatidylcholine, phosphatidylglycerol, phosphatidylinositol, phosphatidylserine, phosphatidylethanolamine, synthetic phospholipids, PEG-ylated phospholipids, phosphorylated lipids, phosphorylated vitamin E and mixtures thereof. 
     
     
         8 . The composition of  claim 1 , wherein the optional other pharmaceutically acceptable ingredients are selected from glycols, trehalose, PCA, NaPCA, a base, selected from pharmaceutically acceptable bases, like but not limited to sodium hydroxide, potassium hydroxide, triethanolamine and ammonia, borax, plasticizers, emollients, sunscreens, pigments, antioxidants, stabilizers, perfumes and combinations thereof. 
     
     
         9 . (canceled) 
     
     
         10 . The composition of  claim 1 , wherein the film-forming ingredient is selected from hydrophilic film-forming ingredients selected from cellulose derivatives, hydroxypropylcellulose, hydroxyethylcellulose, PVP, and combinations thereof. 
     
     
         11 . The composition of  claim 1 , wherein the film-forming ingredient is selected from ethyl cellulose, esters of poly[methylvinyl ether/maleic acid) copolymer, PVP, PVA, PVP/PVA combinations, cationic cellulose polymers, chitosan, chitosan derivatives, polyacrylates, Eudragits, and combinations thereof. 
     
     
         12 . The composition of  claim 1 , in the form of a pharmaceutically acceptable form of administration, selected from a solution, a lotion, a gel, a foam, a patch, a cream, a spray and a spray lacquer. 
     
     
         13 . The composition of  claim 1 , comprising the following components:
 a. 0.01-20% of an antifungal drug selected from, ciclopirox, amorolfine, griseofulvine, posaconazole, butenafine, itraconazole, terbinafine and salts thereof, or other approved antifungal drug and combinations thereof,   b. 0.2-20% w/w of a lipid selected from phospholipids, phosphorylated lipids,   c. 50-90% of a volatile solvent selected from ethanol, isopropanol, n-propanol, butanol, ethyl acetate and combinations thereof,   d. 0-30% of a glycol selected from ethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol, tetraglycol, butylene glycol, hexylene glycol and glycol esters or ethers like ethylene glycol monomethyl ether, diethylene glycol monoethyl ether or other pharmaceutically acceptable glycols and combinations thereof,   e. 0-15% of a film-forming ingredient selected from cellulose derivatives, butyl monoester of poly[methylvinyl ether/maleic acid] copolymer, PVP, PVA, Eudragits, other pharmaceutically acceptable polymers and combinations thereof,   f. 0-40% water,   g. 0-10% of a base, selected from 0.5N to 1.0N aqueous solution of sodium hydroxide, potassium hydroxide, ammonia borax and combinations thereof, and   h. 0-5% of other pharmaceutically acceptable excipients selected from plasticizers, emollients, sunscreens, pigments, antioxidants, stabilizers, perfumes, and combinations thereof.   
     
     
         14 . The composition of  claim 1 , in the form of a topical solution or spray, whereby said solution or spray is capable of being applied to a nail or skin surface with a brush or a metered dose device, thereby forming a film when allowed to dry. 
     
     
         15 . The composition of  claim 1 , wherein the at least one active agent is terbinafine or a pharmaceutically acceptable salt of terbinafine, said composition comprising 0.01-20% terbinafine or a pharmaceutically acceptable salt of terbinafine, 0.2-20% of a phospholipid1 61-90% of volatile solvents selected from C2-C4 alcohols and combinations thereof, 0-40% water, 0-30% of a glycol 10.2-15% of a film-form ng ingredient and optionally 0-5% other pharmaceutically acceptable ingredients, wherein upon application to a nail or skin surface and following the rapid evaporation of the volatiles, a continuous film is formed on the nail or skin surface treated, said film exhibiting a web-like structure comprising terbinafine or salt thereof. 
     
     
         16 - 17 . (canceled) 
     
     
         18 . The composition of  claim 15 , comprising the following components:
 0.01-20% of terbinafine or one or more terbinafine salts,   0.2-20% w/w of a lipid selected from phospholipids, phosphorylated lipids,   61-90% of a volatile solvent selected from ethanol, isopropanol, n-propanol, butanol, ethyl acetate and combinations thereof,   0-30% of a glycol selected from ethylene glycol, diethylene glycol, propylene glycol, dipropylene tetraglycol, butylene glycol, hexylene glycol and glycol esters or ethers like ethylene glycol monomethyl ether, diethylene glycol monoethyl ether or other pharmaceutically acceptable glycols and combinations thereof,   0-10% of a film-forming ingredient selected from cellulose derivatives, butyl monoester of poly[methylvinyl ether/maleic acid copolymer, PVP, PVA, Eudragits, other pharmaceutically acceptable polymers and combinations thereof,   0-40% water,   0-10% of 0.5N to 1.0N aqueous solution of a base selected from sodium hydroxide, potassium hydroxide, ammonia borax and combinations thereof, and   0-5% of other pharmaceutically acceptable excipients, selected from plasticizers, emolients, sunscreens, pigments, antioxidants, stabilizers, perfumes, and combinations thereof.   
     
     
         19 . The composition of  claim 15 , comprising about 10% w/w terbinafine hydrochloride, about 5% w/w of one or more phospholipids, about 0.2% w/w of Vitamin E, about 0.5% w/w Klucel, about 7% w/w of a 1N solution of sodium hydroxide, about 65% w/w ethanol, and water. 
     
     
         20 . The composition of  claim 1 , wherein the active agent is Ibuprofen, said composition comprising 0.3-15% w/w Ibuprofen. 
     
     
         21 . A method of treating a nail or skin fungal infection in a human in need thereof, the method comprising applying to the nail or skin a therapeutically effective dose of the composition of  claim 1 , and allowing the composition to dry, thereby forming a film. 
     
     
         22 . A method of treating nail or skin afflictions, the method comprising contacting the afflicted nail or skin with the composition of  claim 1 , thereby forming an occlusive film over the nail or skin. 
     
     
         23 . An article of manufacture comprising a dispensing device and the composition of  claim 1 , contained therein. 
     
     
         24 . A topical film-forming composition, comprising:
 0.01 to 20% of at least one active agent;   a volatile solvent selected from the group consisting of ethyl acetate and a mixture of ethyl acetate and C2-C4 alcohol, wherein the concentration of said volatile(s) in the composition is from 60 to 90%;   0.2 to 15% film-forming ingredient; and   0.2 to 20% of a phospholipid.   
     
     
         25 . A composition according to  claim 24 , wherein the C2-C4 alcohol is ethanol.