Objective To optimize the formulation of Ginseng fruit saponins procationic liposomes and study on the release and cytotoxicity in vitro. Methods Ginseng fruit saponins procationic liposomes were prepared by the ethanol injection and freeze-drying methods, using Box-Behnken experimental design to optimize the liposomal formulation, using electron microscope to observe morphology of liposomes, using dialysis method for in vitro release study, and MTT method for investigating liposome cytotoxicity. Results The optimal liposome formulation after the Box-Behnken optimization is DOTAP of 329.2 mg, egg phosphatidylcholine of 192.2 mg, cholesterol of 332.2 mg, liposome encapsulation efficiency of 65.29%, after reconstitution the particle size of liposomes was concentrated with a uniform spherical shape; in vitro release test results show that the liposomes have sustained-release effect, to extend the duration of action; liposomes on cell toxicity is small, with better cell security. Conclusion Compared with Ginseng fruit saponins, the procationic liposomes can smoothly release drug and enhance oral bioavailability.%目的 优化人参果皂苷前体阳离子脂质体的处方,并对其体外释放、细胞毒性进行研究.方法 采用乙醇注入法、冷冻干燥法制备人参果皂苷前体阳离子脂质体,用Box-Behnken试验设计优化脂质体处方,扫描电镜观察脂质体的形态,透析法考察脂质体的体外释放度,MTT法考察脂质体细胞毒性.结果 Box-Behnken优化后脂质体最优处方为:DOTAP质量329.2 mg,蛋黄卵磷脂质量192.2 mg,胆固醇质量332.2 mg,脂质体包封率达到65.29%,复溶后的脂质体粒径分布集中,形态均一呈球形;体外释放实验结果表明脂质体具有缓释效果,能够延长作用时间;脂质体对细胞的毒副作用较小,具有较好的细胞安全性.结论 人参果皂苷前体阳离子脂质体与原料药相比具有延缓释放,增强口服生物利用度等特点.
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