Penetrating pharmaceutical foam
View Patent ↗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 a compressed gas propellant, the carrier comprising:
i) a surface-active agent, wherein the surface-active agent is a non-ionic surface-active agent, an ionic surface-active agent, or mixtures thereof, wherein the surface-active agent is selected from the group consisting of a polysorbate, a polyoxyethylene fatty acid ester, a polyoxyethylene alkyl ether, a sucrose ester, a partial ester of sorbitol, a partial ester of sorbitol anhydride, sodium methyl cocoyl taurate, sodium methyl oleoyl taurate, sodium lauryl sulfate, triethanolamine lauryl sulfate, a betaine, a mono-, di- or tri-ester of sucrose with food fatty acids (sucrose esters), a monoglyceride, a diglyceride, polyoxyethylene (20) sorbitan monostearate, polyoxyethylene (20) sorbitan monooleate, polyoxyethylene (8) stearate, polyoxyethylene (20) stearate, polyoxyethylene (100) stearate, a polyoxyethylene cetyl ether, a polyoxyethylene palmityl ether, a polyethylene oxide hexadecyl ether, polyoxyethylene (2) cetyl ether, polyoxyethylene (10) cetyl ether, sorbitan monolaurate, isoceteth-20, cocamidopropyl betaine, polyoxyethylene (40) stearate, and mixtures of any two or more thereof;
ii) about 2% to about 75% by weight of the carrier of a liquid, non-volatile hydrophobic solvent, wherein the hydrophobic solvent is a mixture of octyldodecanol and isopropyl myristate;
iii) a foam adjuvant; and
iv) water;
wherein a breakable foam forms upon dispensing of the foamable composition.
2. The foamable composition of claim 1 , wherein the carrier further comprises a therapeutically effective amount of at least one active agent.
3. The foamable composition of claim 2 , 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.
4. The foamable composition of claim 1 , wherein the liquefied or compressed gas propellant is at a concentration of about 3% to about 18% by weight of the carrier.
5. The foamable composition of claim 1 , wherein the surface-active agent is a mixture of the non-ionic surface-active agent and the ionic surface-active agent.
6. The foamable composition of claim 5 , wherein the ratio of the non-ionic surface-active agent to the ionic surface-active agent is between 1:1to 20:1.
7. The foamable composition of claim 1 , wherein the surface-active agent is a non-ionic surface-active agent.
8. The foamable composition of claim 1 , wherein the surface-active agent is present at about 0.3% to about 6.25% by weight of the carrier.
9. The foamable composition of claim 1 , wherein the carrier is an oil-in-water emulsion.
10. The foamable composition of claim 1 , wherein the carrier further comprises a preservative, a pH adjusting agent, or a mixture thereof.
11. The foamable composition of claim 1 , wherein the carrier further comprises about 2% to about 30% by weight of the carrier of a therapeutic enhancer.
12. The foamable composition of claim 11 , 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.
13. The foamable composition of claim 12 , wherein therapeutic enhancer is contained in the foamable composition in an amount from about 2% to about 10% by weight of the carrier.
14. The foamable composition of claim 1 , wherein the breakable foam has a specific gravity of between about 0.01 and about 0.1.
15. The foamable composition of claim 1 , wherein the carrier further comprises a gelling agent at a concentration of less than 1% by weight of the carrier.
16. The foamable composition of claim 15 , wherein the gelling agent is a carbomer, a hypromellose, or mixtures thereof.
17. The foamable composition of claim 15 , wherein the ratio between the foam adjuvant and the hydrophobic solvent is selected from a group consisting of about 1:12, about 1:24, about 1:44, about 1:60, about 1:25, and about 1:220.
18. The foamable composition of claim 1 , wherein the hydrophobic solvent is included at a concentration of 5% to about 10% or 10% to about 20% by weight of the carrier.
19. The foamable composition of claim 1 , wherein the ratio between the surface-active agent and the hydrophobic solvent is between about 1:8 and about 1:16 or is between about 1:16 and about 1:32.
20. The foamable composition of claim 1 , wherein the surface-active agent is about 0.1% to about 5% by weight of the carrier.
21. The foamable composition of claim 1 , wherein the ratio between the surface-active agent and the hydrophobic solvent is selected from a group consisting of about 3:8, about 2:7, about 2:5, about 2:13, about 1:5, about 1:6, about 1:8, about 1:16, about 1:32, about 1:36, between about 1:8 and about 1:16, and between about 1:16, about 1:32.
22. The foamable composition of claim 1 , wherein the ratio between the gelling agent and the hydrophobic solvent is selected from a group consisting of about 1:10, about 1:16 about 2:15, about 1:24, about 1:20, about 1:55, about 1:41, and about 1:50.
23. The foamable composition of claim 1 , wherein the ratio between the gelling agent and the surface-active agent is selected from a group consisting of about 1:3, about 3:10, about 1:7, about 3:28, about 1:10, about 1:5, about 1:8, and about 2:1.
24. The foamable composition of claim 1 , further comprising a gelling agent.
25. The foamable composition of claim 24 , wherein the carrier further comprises a therapeutically effective amount of at least one active agent.
26. The foamable composition of claim 25 , wherein the active agent is selected from the group consisting of an anti-fungal agent, an anti-viral agent, a steroid, a corticosteroid, an anti-histamine, an immunomodulating agent, an immunosuppressant, an anti-allergic agent, a local anesthetic agent, an insecticide, an insect repellent, an anti-cancer drug, a photodynamic therapy agent, an active agent for burns, wounds, cuts and ulcers, 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.