Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo
Xingyan Liu1, Hong Liu1, Jianqiang Liu2, Zhiwei He1, Congcong Ding1, Guoliang Huang1, Weihua Zhou3, Leshan Zhou3
1China-America Cancer Research Institute, of Guangdong Medical College, 2School of Pharmacy, Guangdong Medical College, Dongguan, Guangdong, People’s Republic of China; 3Central South University, Changsha, Hunan, People’s Republic of China
Background: The purpose of this study was to develop a transdermal ligustrazine patch containing a stable formulation and with good entrapment efficiency, release rate, and transdermal absorption.
Methods: Ligustrazine ethosomes were prepared by ethanol injection-sonication, with entrapment efficiency as an indicator. Using acrylic resin as the primary constituent, the ligustrazine ethosome patch was prepared by adding succinic acid as a crosslinking agent and triethyl citrate as a plasticizer. In vitro release and transdermal permeation studies were carried out. Finally, a pharmacokinetic study was carried out in rats to explore relative bioavailability. The formulations of ligustrazine ethosome were 1% (w/v) phospholipid, 0.4% (w/v) cholesterol, and 45% (v/v) ethanol.
Results: Ligustrazine ethosomes were obtained with an average particle size of 78.71 ± 1.23 nm and an average entrapment efficiency of 86.42% ± 1.50%. In vitro transdermal testing of the ligustrazine ethosome patches showed that the cumulative 24-hour amount of ligustrazine was up to 183 ± 18 µg/cm2. The pharmacokinetic results revealed that the relative bioavailability was 209.45%.
Conclusion: Compared with conventional ligustrazine administration, ligustrazine ethosome patches could promote better drug absorption and increase bioavailability. This study demonstrates that the transdermal action of the ligustrazine ethosome patch was comparatively good.
Keywords: ligustrazine, ethosomes, patch