人参皂苷Rg3脂质体的处方优化及制备工艺研究

Study on Optimization of Formulation and Preparation Process of Ginsenoside Rg3 Liposomes

目的为了提高人参皂苷Rg3的生物利用度和靶向性,以卵磷脂和胆固醇为载体材料,研究人参皂苷Rg3脂质体的处方和制备工艺。方法采用薄膜超声分散法制备脂质体,HPLC测定人参皂苷Rg3的含量。以包封率为指标,采用单因素和正交试验法优选处方和工艺。结果人参皂苷Rg3脂质体的最佳处方和工艺条件为:以氯仿-乙醇(1∶1)为溶剂,卵磷脂、胆固醇、人参皂苷Rg3的质量比为4∶2∶1,载药温度为50℃,PBS缓冲溶液的p H值为7.5。制备的脂质体平均粒径为111.8 nm,包封率为87.85%。结论该工艺方法简便、稳定可行,适用于人参皂苷Rg3脂质体的制备。

Objective To improve the bioavailability and targeting property of ginsenoside Rg3, lecithin and cholesterol were used as the carrier materials to optimize the formulation and preparation technology of ginsenoside Rg3 liposomes.Methods Liposomes were prepared by thin-film ultrasonic dispersion method, and the content of ginsenoside Rg3 was determined by HPLC. With the entrapment efficiency as the observation index, the formulation and process were optimized by single factor investigation and orthogonal test.Results The optimal formulation and process conditions were as follows：the solvent was chloroform-ethanol（1∶1）, the best weight ratio of lecithin to cholesterol and ginsenoside Rg3 was 4∶2∶1,the temperature was 50 ℃,and the pH value of PBS buffer was 7.5. The average particle diameter of the liposomes was 111.8 nm,and the entrapment efficiency was 87.85%.Conclusion The optimized process is feasible,stable and applicable for the production of ginsenoside Rg3 liposomes.