土贝母皂苷甲长循环脂质体的制备及体外性质考察

Study on the Preparation and in Vitro Properties of Tubeimoside A Long-circulating Liposomes

关键词:  土贝母皂苷甲  长循环脂质体  体外释放  体外溶血

Key words:  tubeimoside A  long-circulating liposomes  in vitro release  in vitro hemolysis assay

摘要:

目的 制备土贝母皂苷甲长循环脂质体（tubeimoside A long-circulating liposomes，TA-LC-Lipo），并进行体外性质考察。方法 乙醇注入法制备TA-LC-Lipo；采用HPLC测定包封率及体外释放率；通过Marlvern激光粒径分析仪测定粒径和Zeta电位；肉眼观察法和紫外分光光度法评价其溶血作用。结果 确定处方为大豆磷脂浓度10 mg·mL^-1、药脂比1：10、大豆磷脂：胆固醇=4：1、DSPE-PEG 2000的摩尔含量为5%。制备得到的TA-LC-Lipo的平均粒径、PDI、电位、包封率分别为123.0 nm，0.134，-1.20 mV，86.2%。结论 制得的TA-LC-Lipo粒度分布均匀，包封率较高，有较好的缓释作用，并能有效改善土贝母皂苷甲的溶血现象。

Abstract:

OBJECTIVE To prepare tubeimuside A long-circulating liposomes(TA-LC-Lipo), and to study the in vitro properties of TA-LC-Lipo. METHODS TA-LC-Lipo was prepared by ethanol injection; encapsulation efficiency and in vitro release rate of TA-LC-Lipo were determined by HPLC; particle size and Zeta potential of TA-LC-Lipo were measured by a Marlvern Zetasizer Nano-ZS90; hemolysis of TA-LC-Lipo was assessed by visual observation and UV analysis. RESULTS The optimum prescription was as follows:the concentration of soybean phospholipid(SPC) was 10 mg·mL^-1, the ratio of drug to SPC was 1:10, the ratio of SPC to cholesterol was 4:1, and the molar content of DSPE-PEG 2000 was 5%. The average particle size, PDI, Zeta potential, and encapsulation efficiency of the prepared TA-LC-Lipo were 123.0 nm, 0.134, -1.20 mV, and 86.2%, respectively. CONCLUSION The prepared TA-LC-Lipo shows uniform particle size distribution, high encapsulation efficiency, sustained release, and low hemolytic activity in vitro.