[关键词]
[摘要]
目的 研究甘草次酸(GA)-丹参酮IIA(Tan IIA)复方脂质体(GT-Lip)的制备工艺。方法 以大豆卵磷脂(SPC)和胆固醇(Ch)为膜材,薄膜分散探头超声法制备GT-Lip。通过单因素考察确定水合温度和探头超声功率,正交设计法优化处方工艺;低速离心法测定脂质体中GA与Tan IIA包封率,动态光散射粒径仪测定脂质体粒径与Zeta电位,透射电镜测定脂质体形态。结果 优化处方工艺为SPC-Ch质量比6∶1,SPC-Tan IIA物质的量之比30∶1,SPC-GA物质的量之比24∶1,水合温度为30 ℃,探头超声条件为380 W超声5 min;制备得到的GT-Lip中Tan IIA、GA的包封率分别为(81.50±0.76)%、(98.63±0.90)%(n=3),平均Zeta电位为(?19.00±0.98)mV(n=3),平均粒径为(120.5±1.62)nm(n=3)。结论 优化的GT-Lip制备工艺稳定可行。
[Key word]
[Abstract]
Objective To study the preparation technology of glycyrrhetinic acid (GA)-tanshinone IIA (Tan IIA) compound liposomes (GT-Lip). Methods The compound liposomes were made of soybean phosphatidylcholine (SPC) and cholesterol (Ch) by film dispersion ultrasonic probe method. Hydration temperature and ultrasonic power were optimized by single factor tests and the optimum formulation was selected by orthogonal design. The encapsulation efficiencies (EE) of GA and Tan IIA were determined by low-speed centrifugation. The particle size and Zeta potential of liposomes were detected by dynamic light scattering particle size meter. Transmission electron microscopy was used to observe morphous. Results The optimal preparation conditions were as follows weight ratio of SPC-Ch 6∶1, molar ratio of SPC-Tan IIA and SPC-GA was 30∶1 and 24∶1, hydration temperature 30 ℃, and ultrasonic power 380 W for 5 min. Using the optimal method, the EE values of GA and Tan IIA in GT-Lip were (81.50 ± 0.76)% and (98.63 ± 0.90)% (n = 3), and the average particle size of liposomes was (120.5 ± 1.62) nm and the Zeta potential of liposomes was (?19.00 ± 0.98) mV (n = 3). Conclusion The optimal preparation method of GT-Lip in this study is stable and feasible.
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[基金项目]
国家自然科学基金资助课题(81202928);北京市自然科学基金资助课题(7132118);北京中医药大学复方中药制药研究创新团队项目(2011-CXTD-13)