Penetrating pharmaceutical foam

Abstract

The invention relates to an alcohol-free cosmetic or pharmaceutical foam composition comprising water, a hydrophobic solvent, a surface-active agent, a gelling agent, an active component selected from the group of urea, hydroxy acid and a therapeutic enhancer and a propellant. The foam further comprises active agents and excipients with therapeutic properties having enhanced skin penetration.

1 . A foamable composition comprising a carrier and a liquefied or compressed gas propellant, the carrier comprising:
 i) about 0.1% to about 5% by weight of the carrier of a foam adjuvant;   ii) about 2% to about 75% by weight of the carrier of a liquid, volatile hydrophobic solvent; and   iii) water; and   iv) optionally about 0.1% to about 5% by weight of the carrier of a gelling agent selected from the group consisting of: a micro-crystalline cellulose, a carboxyvinyl polymer, a polyvinylpyrrolidone, a polyvinyl alcohol polyacrylic acid polymer, a polymethacrylic acid polymer, a polyvinyl acetate polymer, a polyvinyl chloride polymer, a polyvinylidene chloride polymer, an acrylic acid copolymer, an ethyl acrylate copolymer, a synthetic polymeric material, a carboxyvinyl polymer, an amphiphilic copolymer, and mixtures of any two or more thereof; and   wherein the liquefied or compressed gas propellant is at a concentration of about 3% to about 18% by weight of the total composition; wherein the composition contains no more than 7.5% by weight of methyl alcohol, ethyl alcohol, isopropyl alcohol, butyl alcohol, or mixtures thereof; and wherein a breakable foam forms upon dispensing the foamable composition.   
     
     
         2 . The foamable composition of  claim 1 , wherein the carrier comprises a gelling agent, and wherein the gelling agent comprises an acrylic acid copolymer, a carboxyvinyl polymer, or a mixture thereof. 
     
     
         3 . The foamable composition of  claim 1 , wherein the ratio of the foam adjuvant to the hydrophobic solvent is between about 1:12 and about 1:44. 
     
     
         4 . The foamable composition of  claim 1 , wherein the carrier comprises a gelling agent, and wherein the ratio of the gelling agent to the hydrophobic solvent is between about 1:24 and about 1:36. 
     
     
         5 . The foamable composition of  claim 1 , wherein the volatile hydrophobic solvent is a volatile silicone oil. 
     
     
         6 . The foamable composition of  claim 1 , wherein the carrier further comprises a surface active agent at a concentration of about 0.1% to about 5% by weight of the carrier, wherein the surface active agent is a mixture of a non-ionic surface active agent and an ionic surface active agent, and wherein the ratio of the non-ionic surface active agent to the ionic surface active agent is between about 1:1 and about 20:1. 
     
     
         7 . The foamable composition of  claim 1 , wherein the carrier further comprises a therapeutically effective amount of at least one active agent, and a therapeutic enhancer. 
     
     
         8 . A foamable composition comprising a carrier and a liquefied or compressed gas propellant, the carrier comprising:
 i) about 2% to about 75% by weight of the carrier of a liquid, volatile hydrophobic solvent;   ii) a therapeutically effective amount of at least one active agent;   iii) a therapeutic enhancer;   iv) about 0.1% to about 5% by weight of the carrier of a foam adjuvant;   v) water; and   vi) about 0.1% to about 5% by weight of the carrier of a gelling agent selected from the group consisting of: a micro-crystalline cellulose, a carboxyvinyl polymer, a polyvinylpyrrolidone, a polyvinyl alcohol polyacrylic acid polymer, a polymethacrylic acid polymer, a polyvinyl acetate polymer, a polyvinyl chloride polymer, a polyvinylidene chloride polymer, an acrylic acid copolymer, an ethyl acrylate copolymer, a synthetic polymeric material, a carboxyvinyl polymer, an amphiphilic copolymer, and mixtures of any two or more thereof;   wherein the liquefied or compressed gas propellant is at a concentration of about 3% to about 18% by weight of the total composition; wherein the composition contains no more than 7.5% by weight of methyl alcohol, ethyl alcohol, isopropyl alcohol, butyl alcohol, or mixtures thereof; and wherein a breakable foam forms upon dispensing of the foamable composition.   
     
     
         9 . The foamable composition of  claim 8 , wherein the active agent is selected from the group consisting of an antibacterial agent, an anti-fungal agent, an anti-viral agent, an anti-inflammatory agent, a steroid, a corticosteroid, an anti-histamine, a nonsteroidal anti-inflammatory agent, an immunomodulating agent, an immunosuppressant, an anti-allergic agent, a local anesthetic agent, a retinoid, an insecticide, an insect repellent, an anti-cancer drug, a photodynamic therapy agent, an active agent for burns, wounds, cuts and ulcers, an anti-acne active agent, an anti-wrinkle active agent, an anti-atrophy active agent, an anti-oxidant, a radical scavenger, a self-tanning active agent, a skin lightening or whitening agent, an agent suitable for the treatment of a hair growth disorder, an agent for treating cellulite, and mixtures of any two or more thereof. 
     
     
         10 . The foamable composition of  claim 8 , wherein the therapeutic enhancer is at a concentration of about 2% to about 30% by weight of the carrier. 
     
     
         11 . The foamable composition of  claim 8 , wherein the therapeutic enhancer is selected from the group consisting of a polyhydric alcohol, propylene glycol, butylene glycol, glycerol, pentaerythritol, sorbitol, mannitol, an oligosaccharide, dimethyl isosorbide, monooleate of ethoxylated glycerides with 8 to 10 ethylene oxide units, a polyethylene glycol 200-600, diethylene glycol monoethyl ether, glycofurol, a cyclodextrin, and mixtures of any two or more thereof. 
     
     
         12 . The foamable composition of  claim 8 , wherein the gelling agent comprises an acrylic acid copolymer, a carboxyvinyl polymer, or a mixture thereof. 
     
     
         13 . The foamable composition of  claim 8 , wherein the ratio of the foam adjuvant to the hydrophobic solvent is between about 1:12 and about 1:44. 
     
     
         14 . The foamable composition of  claim 8 , wherein the ratio of the gelling agent to the hydrophobic solvent is between about 1:24 and about 1:36. 
     
     
         15 . The foamable composition of  claim 8 , wherein the volatile hydrophobic solvent is a volatile silicone oil. 
     
     
         16 . The foamable composition of  claim 15 , wherein the volatile silicone oil is a cyclomethicone. 
     
     
         17 . The foamable composition of  claim 8 , wherein the carrier further comprises a surface active agent at a concentration of about 0.1% to about 5% by weight of the carrier, wherein the surface active agent is a mixture of a non-ionic surface active agent and an ionic surface active agent, and wherein the ratio of the non-ionic surface active agent to the ionic surface active agent is between about 1:1 and about 20:1. 
     
     
         18 . A method of applying a breakable foam to a targeted skin or mucosal surface of a subject, comprising
 a. dispensing the foamable composition of  claim 8  to the targeted skin or mucosal surface; and   b. spreading or collapsing the foam by applying mechanical force to the breakable foam.   
     
     
         19 . The method of  claim 18 , wherein the active agent is selected from the group consisting of an antibacterial agent, an anti-fungal agent, an anti-viral agent, an anti-inflammatory agent, a steroid, a corticosteroid, an anti-histamine, a nonsteroidal anti-inflammatory agent, an immunomodulating agent, an immunosuppressant, an anti-allergic agent, a local anesthetic agent, a retinoid, an insecticide, an insect repellent, an anti-cancer drug, a photodynamic therapy agent, an active agent for burns, wounds, cuts and ulcers, an anti-acne active agent, an anti-wrinkle active agent, an anti-atrophy active agent, an anti-oxidant, a radical scavenger, a self-tanning active agent, a skin lightening or whitening agent, an agent suitable for the treatment of a hair growth disorder, an agent for treating cellulite, and mixtures of any two or more thereof. 
     
     
         20 . The method of  claim 18 , wherein the gelling agent is selected from the group consisting of: an acrylic acid copolymer, a carboxyvinyl polymer, and a mixture thereof. 
     
     
         21 . The method of  claim 18 , wherein the volatile hydrophobic solvent is a volatile silicone oil. 
     
     
         22 . The method of  claim 18 , wherein the foamable composition further comprises a surface active agent at a concentration of about 0.1% to about 5% by weight of the carrier, wherein the surface active agent is a mixture of a non-ionic surface active agent and an ionic surface active agent, and wherein the ratio of the non-ionic surface active agent to the ionic surface active agent is between about 1:1 and about 20:1.