Synergistic penetration of ethosomes and lipophilic prodrug on the transdermal delivery of acyclovir.
The aim of this study was to investigate the lipophilic prodrug as a means of promoting acyclovir (ACV) that exhibited biphasic insolubility into the ethosomes for optimum skin delivery. Acyclovir Palmitate (ACV-C(16)) was synthesized as the lipophilic prodrug of ACV. The ethosomal system and the liposomal system bearing ACV or ACV-C(16) were prepared, respectively. The systems were characterized for shape, zeta potential value, particle size, and entrapment efficiency. Franz diffusion cells and confocal laser scanning microscopy were used for the percutaneous absorption studies. The results showed that the entrapment efficiency of ACV-C(16) ethosomes (87.75%) were much higher than that of ACV ethosomes (39.13%). The quantity of drug in the skin from ACV-C(16) ethosomes at the end of the 24 h transdermal experiment (622.89 microg/cm(2)) was 5.30 and 3.43 times higher than that from ACV-C(16) hydroalcoholic solution and ACV ethosomes, respectively. This study indicated that the binary combination of the lipophilic prodrug ACV-C(16) and the ethosomes synergistically enhanced ACV absorption into the skin.
Zhou
Yan
Y
Department of Pharmacy, 1st Hospital of Lanzhou University, Lanzhou, 730000, China.
Wei
Yu-Hui
YH
Zhang
Guo-Qiang
GQ
Wu
Xin-An
XA
D000212:Acyclovir / Q000008:administration & dosage* / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage* / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000737:chemistry*; D004357:Drug Synergism; D005260:Female; D066298:In Vitro Techniques; D008081:Liposomes; D051379:Mice; D008815:Mice, Inbred Strains; D018613:Microscopy, Confocal; D046529:Microscopy, Electron, Transmission; D010168:Palmitates / Q000737:chemistry*; D010316:Particle Size; D011355:Prodrugs / Q000008:administration & dosage*; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility
D000998:Antiviral Agents; D004337:Drug Carriers; D008081:Liposomes; D010168:Palmitates; D011355:Prodrugs; D000212:Acyclovir