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[摘要]
摘 要:目的 研究甘草次酸-丹参酮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甘草次酸(GA)-丹参酮IIA(TSN)复方脂质体。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TSN 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-TSN 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TSN、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±0.98)mV(n=3),平均粒径为(120.5±1.62) nm(n=3)。结论 所得优化工艺制备GT-Lip 稳定可行。
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[Abstract]
Abstract: Objective To study the preparation method of glycyrrhetinic acid-tanshinone IIA compound liposomes (GT-Lip). Methods Liposomes were made of cholesterol (CH) and soybean phosphatidylcholine (SPC) by film-ultrasound technique. After the exploration of single factors including hydration temperature and ultrasonic power, orthogonal design was used to select the optimum formulation. The particle size and zeta potential of liposomes were detected by Zetasizer Nano, while the encapsulation efficiencies of glycyrrhetinic acid (GA) and tanshinone IIA (TSN) were simultaneously determined by RP-HPLC after the liposomes and freed drugs were separated by low-speed centrifugation. Results The optimal preparation conditions were as follows: SPC-CH 6∶1 w/w, SPC-TSN 30∶1 mol/mol, SPC-GA 24∶1 mol/mol, hydration temperature 30 ℃, ultrasonic power 380 W. Using the optimal method, the encapsulation efficiencies of GA and TSN were (81.50 ± 0.76)%, (98.63 ± 0.90)% (n = 3) , the particle size of liposomes was 120.5 nm and the Zeta potential of liposomes was (?19 ± 0.98) mV (n=3). Conclusion The optimal preparation method of glycyrrhetinic acid-tanshinone IIA compound liposomes in this study is stable and feasible.
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[基金项目]
基金项目:国家自然科学基金课题(81202928);北京市自然科学基金课题(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)