Box-Behnken优化黄芩苷脂质体的制备工艺及体外释放模型拟合的研究

Preparation Process and in vitro Release Model of Baicalin Liposomes Optimized by Box-Behnken-Response Surface Methodology Design

目的:探讨黄芩苷脂质体的制备工艺,并考察体外释放情况。方法:采用逆向蒸发法、乙醚注入法、薄膜分散法制备脂质体,以包封率和粒径作为考察指标,通过单因素试验和Box-Behnken响应面法优选最佳处方工艺,并对黄芩苷脂质体的体外释放应用各模型进行拟合。结果:最佳处方为:磷脂药物比为3.81∶1,磷脂胆固醇比为5.70∶1,水化体积为1.02 mL,测得黄芩苷脂质体的平均包封率为44.16%,粒径160~190 nm。结论:逆向蒸发法制备的黄芩苷脂质体包封率最高,黄芩苷脂质体体外释药具有双相动力学特征。

Objective：To investigate the preparation technology of baicalin liposomes and investigate its in vitro release. Methods： Baicalin liposomes were prepared by reverse evaporation method, injection method and membrane ultrasound method. The best prescription process was selected by single factor experiment and Box-Behnken Design-Response Surface Methodology with entrapment efficiency and particle size as the indexes,the in vitro release of baicalin liposomes was simulated by different models. Results：The best prescription was phospholipid and drug ratio at 3.81： 1, phospholipid and cholesterol ratio was 5.70：1, hydration volume was 1.02 mL, the average encapsulation efficiency of baicalin liposomes was 44. 16% and the particle size was 160- 190 nm. Conclusion：Baicalin liposomes prepared by reverse evaporation has the highest entrapment efficiency,and the release of baicalin liposomes has biphasic kinetic characteristics.