橙皮苷脂质体凝胶的制备及其透皮吸收研究

目的:制备橙皮苷脂质体凝胶并对其体外释药和透皮吸收情况进行考察。方法:采用薄膜超声法制备橙皮苷脂质体,以包封率为主要评价指标,在单因素实验基础上采用Box-Behnken响应面法优化处方,并对最优处方制备的橙皮苷脂质体凝胶进行各项理化指标、体外释放模型和透皮吸收进行考察。结果:橙皮苷脂质体最优处方为磷胆比2.35∶1、磷药比7.43∶1、水合介质pH 6.54。橙皮苷脂质体粒径(207.87±13.27)nm,PDI (0.36±0.02),Zeta电位(-40.60±3.32)mV,包封率(58.21±0.90)%,橙皮苷脂质体凝胶体外释药曲线符合Ritger-Peppas方程(R²_adj=0.998 9)。结论:橙皮苷脂质体凝胶黏度适宜,易于涂展,体外释药具有明显的缓释效果且透皮吸收特性良好,该制备方法稳定可行,适用于橙皮苷脂质体凝胶的制备。

Preparation and transdermal absorption of hesperidin liposome gel

OBJECTIVE To prepare hesperidin liposome gel, and investigate its in vitro drug release and transdermal absorption.METHODS Hesperidin liposome was prepared by thin film ultrasonic method. The formulation was optimized by Box-Behnken response surface methodology with entrapment efficiency as the main evaluation indicator. The physical and chemical indicators, in vitro release model and transdermal absorption of hesperidin liposome gel prepared by the optimal formulation were investigated.RESULTS The optimal formulation of hesperidin liposome was as follows: the ratio of lipid to cholesterol was 2.35∶1, the ratio of lipid to drug was 7.43∶1, and the pH of the hydration medium was 6.54. The particle size of hesperidin liposome was (207.87±13.27) nm, PDI was (0.36±0.02), zeta potential was (-40.60±3.32) mV, entrapment efficiency was (58.21±0.90)%, and the external release curve of hesperidin liposome gel conformed to the Ritger-Peppas equation (R²_adj = 0.998 9).CONCLUSION Hesperidin liposome gel has suitable viscosity, which is easy to spread, and it has obvious sustained release effect and good transdermal absorption characteristics in vitro. The preparation method is stable and feasible, and suitable for the preparation of hesperidin liposome gel.