In vivo microdialysis for the evaluation of transfersomes as a novel transdermal delivery vehicle for cinnamic acid.
In this study, cinnamic acid-loaded transfersomes were prepared and dermal microdialysis sampling was used in Sprague-Dawley rats to compare the amount of drug released into the skin using transfersomes as transdermal carriers with that released on using conventional liposomes. The formulation of cinnamic acid-loaded transfersomes was optimized by a uniform design through in vitro transdermal permeation studies. Hydration time was confirmed as a significant factor influencing the entrapment efficiency of transfersomes, further affecting their transdermal flux in vitro. The fluxes of cinnamic acid from transfersomes were all higher than those from conventional liposomes, and the flux from the optimal transfersome formulation was 3.01-fold higher than that from the conventional liposomes (p < 0.05). An in vivo microdialysis sampling method revealed that the dermal drug concentrations from transfersomes applied on various skin regions were much lower than those required with conventional liposomes. After the administration of drug-containing transfersomes and liposomes on abdominal skin regions of rats for a period of 10 h, the Cmax of cinnamic acid from the compared liposomes was 3.21 ± 0.25 μg/mL and that from the transfersomes was merely 0.59 ± 0.02 μg/mL. The results suggest that transfersomes can be used as carriers to enhance the transdermal delivery of cinnamic acid, and that these vehicles may penetrate the skin in the complete form, given their significant deformability.
School of Pharmacy, Shanghai University of Traditional Chinese Medicine , Shanghai , China.
Yong-Tai
YT
Zhang
Yue-Ming
YM
Xu
Su-Juan
SJ
Zhang
Ji-Hui
JH
Zhao
Zhi
Z
Wang
Ding-Qin
DQ
Xu
Nian-Ping
NP
Feng
D000279:Administration, Cutaneous; D000818:Animals; D002626:Chemistry, Pharmaceutical; D002934:Cinnamates / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D008081:Liposomes; D008297:Male; D017551:Microdialysis / Q000379:methods*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption
D002934:Cinnamates; D008081:Liposomes; C029010:cinnamic acid