Optimization and evaluation of pluronic lecithin organogels as a transdermal delivery vehicle for sinomenine

Abstract

The purpose of the present study was to prepare and optimize sinomenine (SIN) pluronic lecithin organogels system (PLO), and to evaluate the permeability of the optimized PLO in vitro and in vivo. Box–Behnken design was used to optimize the PLO and the optimized formulation was pluronic F127 of 19.61%, lecithin of 3.60% and SIN of 1.27%. The formulation was evaluated its skin permeation and drug deposition both in vitro and in vivo compared with gel. Permeation and deposition studies of PLO were carried out with Franz diffusion cells in vitro and with microdialysis in vivo. In vitro studies, permeation rate (J_ss) of SIN from PLO was 146.55 ± 2.93 μg/cm²/h, significantly higher than that of gel (120.39 μg/cm²/h) and the amount of SIN deposited in skin from the PLO was 10.08 ± 0.86 μg/cm², significantly larger than that from gel (6.01 ± 0.04 μg/cm²). In vivo skin microdialysis studies showed that the maximum concentration (C_max) of SIN from PLO in “permeation study” and “drug-deposition study” were 150.27 ± 20.85 μg/ml and 67.95 μg/ml, respectively, both significantly higher than that of SIN from gel (29.66 and 6.73 μg/ml). The results recommend that PLO can be used as an advantageous transdermal delivery vehicle to enhance the permeation and skin deposition of SIN.

• Box–Behnken design
• microdialysis
• percutaneous permeation
• pluronic lecithin organogels
• sinomenine

Declaration of interest

The authors report no declarations of interest (monetary or otherwise) in conducting this research. The authors alone are responsible for the content and writing of the article. This study was financially supported by the University-industry Cooperation Projects of Ministry of education and Guangdong province (grant No. 2012B091100486) and the Special Funds from Central Finance of China in Support of the Development of Local Colleges and University [grant No. 276 (2014)].