Topical composition comprising a film-forming polymer for delivering an active ingredient to skin

Abstract

A film-forming pharmaceutical composition for dermal application comprises at least one therapeutically active ingredient dissolved in a volatile solvent, the composition further comprising a film-forming polymer, a plasticizer and an oily release-enhancing agent. The composition is capable of forming, after application on skin and evaporation of the solvent, a continuous phase comprising the film-forming polymer and the plasticizer and a dispersed phase comprising droplets of the oily release-enhancing agent.

What is claimed is: 
     
         1 . A film-forming pharmaceutical composition for dermal application, the composition comprising at least one therapeutically active ingredient dissolved in a pharmaceutically acceptable volatile solvent which is present in an amount of 50-99.5% w/w of the composition, the composition further comprising a film-forming polymer in an amount of 0.1-50% w/w, a plasticizer in an amount of 0.1-10% w/w, and medium chain triglycerides as an oily release-enhancing agent in an amount of 0.1-15% w/w;
 the composition being capable of forming, after application on skin and evaporation of the solvent, a continuous phase comprising the film-forming polymer and the plasticizer and a dispersed phase comprising droplets of medium chain triglycerides.   
     
     
         2 . A composition according to  claim 1 , wherein the film-forming polymer is selected from the group consisting of cellulose derivatives, acrylic polymers, acrylic copolymers, methacrylate polymers, methacrylate copolymers, polyurethanes, polyvinylalcohol or a derivative thereof such as polyvinylacetate, silicone polymers and silicone copolymers, or copolymers thereof. 
     
     
         3 . A composition according to  claim 2 , wherein the cellulose derivative is selected from the group consisting of ethyl cellulose, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose. 
     
     
         4 . A composition according to  claim 2 , wherein the acrylic polymer is selected from the group consisting of methyl methacrylate and butyl methacrylate copolymer, ethyl acrylate and methyl methacrylate copolymer, acrylate and ammonium methacrylate copolymer type A and type B, and acrylates/octylacrylamide copolymer. 
     
     
         5 . A composition according to  claim 1 , wherein the amount of film-forming polymer is 5-20% w/w. 
     
     
         6 . A composition according to  claim 1 , wherein the plasticizer is selected from the group consisting of triethyl citrate, tributyl citrate, acetyl triethyl citrate, triacetin, dibutyl sebacate and polyethylene glycol 100-1000. 
     
     
         7 . A composition according to  claim 1 , wherein the amount of plasticizer is 2-5% w/w. 
     
     
         8 . A composition according to  claim 1 , wherein the amount of medium chain triglycerides is 1-10% w/w. 
     
     
         9 . A composition according to  claim 1 , wherein the volatile solvent is a lower alcohol such as methanol, ethanol, n-propanol, isopropanol or butanol, a C 1-4  ester of a C 1-4  carboxylic acid such as methyl acetate, ethyl acetate, butyl acetate, methyl formate or propyl propionate, acetone, or a volatile silicone oil such as cyclomethicone, dimethicone or hexamethyldisiloxane. 
     
     
         10 . A composition according to  claim 1 , wherein the amount of the volatile solvent is 70-80% w/w or 80-90% w/w. 
     
     
         11 . A composition according to  claim 1  further comprising an anti-nucleating agent. 
     
     
         12 . A composition according to  claim 11 , wherein the anti-nucleating agent is selected from the group consisting of polyvinyl alcohol, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, methyl cellulose, polyvinylpyrrolidone and carboxymethyl cellulose. 
     
     
         13 . A composition according to  claim 1  which is substantially anhydrous. 
     
     
         14 . A composition according to  claim 1 , wherein the therapeutically active ingredient is selected from the group consisting of vitamin D derivatives or analogues, corticosteroids, phosphodiesterase 4 inhibitors, ingenol derivatives, retinoids, MK inhibitors, NK-1 receptor antagonists, calcineurin inhibitors, keratolytic agents, antibiotics, non-steroidal antiinflammatory agents and local anesthetics. 
     
     
         15 . A method of treating a dermatological disease or condition, the method comprising applying a composition of  claim 1  on the skin of a patient in need such treatment. 
     
     
         16 . The method of  claim 15 , wherein the dermatological disease or condition is selected from the group consisting of psoriasis, pustulosis palmoplantaris, ichtyosis, atopic dermatitis, contact dermatitis, eczema, actinic keratosis, pruritus, rosacea and acne. 
     
     
         17 . A composition according to  claim 4 , wherein the acrylic polymer is ethyl acrylate and methyl methacrylate copolymer. 
     
     
         18 . A composition according to  claim 5 , wherein the amount of film-forming polymer is 10-15% w/w. 
     
     
         19 . A composition according to  claim 6 , wherein the plasticizer is tributyl citrate. 
     
     
         20 . A composition according to  claim 8 , wherein the amount of medium chain triglycerides is 2-6% w/w.