Enhancement of the skin permeation of clindamycin phosphate by Aerosol OT/1-butanol microemulsions.
Microemulsions of water/isopropyl palmitate (IPP)/Aerosol OT (AOT)/1-butanol were developed as alternative formulations for topical delivery of clindamycin phosphate. Effect of AOT:1-butanol ratios on microemulsion region existence in the pseudoternary phase diagrams was investigated. The 2:1 AOT:1-butanol provided the largest microemulsion region. Five microemulsions of 1% w/w clindamycin phosphate were prepared and characterized. The permeation through human epidermis of the microemulsions was evaluated and compared with the 70% isopropanol solution using modified Franz diffusion cells. The drug permeation from all microemulsions was found to be significantly greater than that from the solution, indicating the enhancement of the skin permeation by the microemulsions. Within the same microemulsion type, the drug permeation increased with increasing the amount of AOT:1-butanol. The drug permeation from oil-in-water (o/w) microemulsions was relatively higher than that from water-in-oil (w/o) microemulsions. In addition, all microemulsions were stable for at least three months at 30 +/- 1 degrees C.
Junyaprasert
Varaporn Buraphacheep
VB
Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand. pyvbp@mahidol.ac.th
Boonsaner
Panee
P
Leatwimonlak
Sujitra
S
Boonme
Prapaporn
P
D020001:1-Butanol / Q000737:chemistry / Q000494:pharmacology*; D000279:Administration, Cutaneous; D000336:Aerosols; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D002981:Clindamycin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D004143:Dioctyl Sulfosuccinic Acid / Q000737:chemistry / Q000494:pharmacology*; D004337:Drug Carriers; D004655:Emulsions; D004817:Epidermis / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D010539:Permeability; D044367:Phase Transition; D012869:Skin Absorption / Q000187:drug effects*; D013501:Surface-Active Agents / Q000737:chemistry / Q000494:pharmacology*
D000336:Aerosols; D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D004655:Emulsions; D013501:Surface-Active Agents; D004143:Dioctyl Sulfosuccinic Acid; D002981:Clindamycin; D020001:1-Butanol; C007084:clindamycin phosphate