绞股蓝总皂苷脂质体的制备与表征

Preparation and characterization of gypenosides liposomes consisted by lecithin and stigmasterol

目的探讨用豆甾醇替代胆固醇制备绞股蓝总皂苷脂质体的可行性,并获得最佳制备工艺与处方。方法以卵磷脂和豆甾醇为膜材制备不含胆固醇的绞股蓝总皂苷脂质体;脂质体以鱼精蛋白沉淀法进行包封率的测定;以包封率为评定指标,筛选该新型绞股蓝总皂苷脂质体的最佳制备方法;采用正交设计优化该脂质体的制备工艺;采用粒径、Zeta电位、原子力显微镜(AFM)表征该新型绞股蓝总皂苷脂质体。结果用豆甾醇替代胆固醇制备绞股蓝总皂苷脂质体的最佳制备方法为乙醇注入法,通过正交设计得最佳工艺为绞股蓝总皂苷与卵磷脂的质量比为1∶10,卵磷脂与豆甾醇的质量比为4∶1,PBS缓冲溶液pH值为7.0,水化温度为35℃;所得脂质体的包封率为(77.00±1.17)%,粒径为(202.6±3.9)nm,多分散系数(PDI)为0.108±0.003,电位为(28.66±0.86)mV,该脂质体在电镜下呈规则圆形。结论用豆甾醇替代胆固醇制备绞股蓝总皂苷脂质体方法可行,采用最佳工艺制备的绞股蓝总皂苷包封率高,形态和粒径均较好,重现性好。

Objective To study the feasibility of preparing gypenoside liposomes （GLs） with stigmasterol instead of cholesterol, and to optimize the prescription and preparation of GLs. Methods GLs without cholesterol were prepared by ethanol injection method with lecithin and stigmasterol, and the encapsulation efficiency was determined by protamine precipitation method. The encapsulation efficiency was adopted to evaluate and optimize the preparation process as response in orthogonal design assay. GLs were characterized by Dynamic Light Scattering and Atomic Force Microscope （AFM） using particle size and electric potential as indexes. Results Ethanol injection was the best method to prepare GLs with lecithin and stigmasterol. The optimal preparation process determined by orthogonal design assay was as follows： the ratio of gypenosides to lecithin was 1︰10, the ratio of lecithin to stigmasterol was 4︰1, the pH value of PBS buffer solution was 7.0, and the hydration temperature was 35 ℃. The entrapment efficiency was （77.00 ± 1.17）%, the particle size was （202.6 ± 3.9） nm, the PDI was 0.108 ± 0.003, the zeta potential was （？28.66 ± 0.86） mV, and the morphology was round observed by AFM. Conclusion The preparation of GLs with lecithin and stigmasterol was feasible. The GLs prepared by optimum preparation process have high encapsulation efficiency, good morphology, and reproducibility.