Nsaid formulations, based on highly adaptable aggregates, for improved transport through barriers and topical drug delivery

A method for inducing analgesia comprising applying to the skin of a warm blooded mammal a vesicular composition comprising:

• a) vesicles having a lipid bilayer and consisting essentially of:
• i) a phosphatidylcholine;
• ii) a polyethyleneglycol-sorbitan-monooleate, a polyoxyethylene-oleoyl ether, or a nonaethyleneglycoloctylphenyl ether surfactant;
• and
• iii) a salt of an NSAID wherein said NSAID is diclofenac, ibuprofen or ketoprofen;
• and
• 2) a pharmaceutically acceptable, polar liquid medium,
• wherein
• the phosphatidylcholine and the surfactant of the vesicles are present in a molar ratio of between about 20/1 and about 7.5/1,
• the molar ratio of phosphatidylcholine to NSAID is between about 10/1 to about 1/1,
• the lipid bilayer is in the fluid lamellar phase, and
• the pH of the composition is above the pKa of the NSAID.

A method for inducing analgesia comprising applying to the skin of a warm blooded mammal a vesicular composition comprising:

• 1) vesicles consisting essentially of:
• i) a phosphatidylcholine;
• ii) a polyethyleneglycol-sorbitan-monooleate, a polyoxyethylene-oleoyl ether, or a nonaethyleneglycoloctylphenyl ether surfactant;
• and
• iii) a salt of an NSAID wherein said NSAID is diclofenac, ibuprofen or ketoprofen;
• and
• 2) a pharmaceutically acceptable, polar liquid medium,
• wherein
• the phosphatidylcholine and the surfactant of the vesicles are present in a molar ratio of between about 20/1 and about 7.5/1,
• the molar ratio of phosphatidylcholine to NSAID is between about 10/1 to about 1/1,
• the vesicles are capable of penetrating a barrier with pores having an average pore diameter at least 50% smaller than the average vesicle diameter before the penetration, and
• the pH of the composition is above the pKa of the NSAID.