A novel vesicular carrier, transethosome, for enhanced skin delivery of voriconazole: characterization and in vitro/in vivo evaluation.
This study describes a novel carrier, transethosome, for enhanced skin delivery of voriconazole. Transethosomes (TELs) are composed of phospholipid, ethanol, water and edge activator (surfactants) or permeation enhancer (oleic acid). Characterization of the TELs was based on results from recovery, particle size, transmission electron microscopy (TEM), zeta potential and elasticity studies. In addition, skin permeation profile was obtained using static vertical diffusion Franz cells and hairless mouse skin treated with TELs containing 0.3% (w/w) voriconazole, and compared with those of ethosomes (ELs), deformable liposomes (DLs), conventional liposomes (CLs) and control (polyethylene glycol, PG) solutions. The recovery of the studied vesicles was above 90% in all vesicles, as all of them contained ethanol (7-30%). There was no significant difference in the particles size of all vesicles. The TEM study revealed that the TELs were in irregular spherical shape, implying higher fluidity due to perturbed lipid bilayer compared to that of other vesicles which were of spherical shape. The zeta potential of vesicles containing sodium taurocholate or oleic acid showed higher negative value compared to other vesicles. The elasticities of ELs and TELs were much higher than that of CLs and DLs. Moreover, TELs dramatically enhanced the skin permeation of voriconazole compared to the control and other vesicles (p<0.05). Moreover, the TELs enhanced both in vitro and in vivo skin deposition of voriconazole in the dermis/epidermis region compared to DLs, CLs and control. Therefore, based on the current study, the novel carrier TELs could serve as an effective dermal delivery for voriconazole.
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, South Korea.
Chung Kil
CK
Song
Prabagar
P
Balakrishnan
Chang-Koo
CK
Shim
Suk-Jae
SJ
Chung
Saeho
S
Chong
Dae-Duk
DD
Kim
D000279:Administration, Cutaneous; D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods*; D004548:Elasticity; D008081:Liposomes; D008297:Male; D051379:Mice; D008812:Mice, Hairless; D011743:Pyrimidines / Q000008:administration & dosage* / Q000494:pharmacology*; D012867:Skin / Q000187:drug effects*; D012869:Skin Absorption / Q000187:drug effects; D014230:Triazoles / Q000008:administration & dosage* / Q000494:pharmacology*; D065819:Voriconazole
D004337:Drug Carriers; D008081:Liposomes; D011743:Pyrimidines; D014230:Triazoles; D065819:Voriconazole