正交试验优选油茶皂苷脂质体的制备工艺

Preparation Process of Sasanquasaponin(SQS) Liposomes by Orthogonal Design

目的优选油茶皂苷脂质体的制备工艺。方法薄膜分散-硫酸铵梯度法制备油茶皂苷脂质体,以包封率为指标,单因素试验确定以磷脂-胆固醇之比、磷脂-药物之比和超声时间为考察因素,通过正交设计优化处方工艺,透析法分离-紫外分光光度法测定包封率。结果最佳制备工艺:磷脂-胆固醇之比4∶1、磷脂-药物之比20∶1和超声时间10min,包封率均值为73.3%。结论优化后的工艺可提高油茶皂苷脂质体的包封率,此工艺条件简单,可操作性强,适于实验室条件下制备油茶皂苷脂质体。

OBJECTIVE To optimize the preparation technology of Sasanquasaponin（ SQS）. METHODS The SQS liposome was prepared by film ultrasonic-ammonium sulfate gradient method. The preparation technology was optimized by orthogonal design with encapsulation coefficency as index using the ratio of phospholipid to cholesterin,the ratio of lipid to drug,the time of probe ultrassonic as factors. Free drug was separated by Sephadex gel and the encapsulalion efficiency of matrine was determined by ultraviolet spectroscopy（ UV-VIS）. RESULTS The optimized preparation conditions for SQS phytosomes were obtained as follows： The ratio of phospholipid to cholesterin was 4∶1,the ratio of lipid to drug was 20 ∶ 1 and the time of probe ultrassonic was 10 min,envelopment percentage was73. 3%. CONCLUSION The entrapment efficiency of liposome could be obviously improved with the optimized condition. The method discussed above was simple,feasible,and easily operated,which could be suitable for laboratory to prepare SQS liposome.