复方鸦胆子油脂质体的制备工艺研究

Study on Prescription and Preparation of Compound Oleum Fructus Bruceae Liposomes

目的:研究复方鸦胆子油脂质体的处方筛选及制备工艺。方法:采用气相色谱法测定脂质体包封率。以脂质体包封率为主要指标,对制备工艺中可能影响脂质体性质的工艺参数和处方因素进行单因素考察和正交设计,优化制备工艺。用不同冻干保护剂进行冷冻干燥,以筛选合适的保护剂。测定Zeta电位、粒径大小及分布。结果:采用乙醇注入法制备复方鸦胆子油脂质体;最佳制备工艺为磷脂浓度为1.5%,磷脂胆固醇质量比为5∶1,油水两相体积比为1∶10,甘露醇∶蔗糖∶磷脂质量比为1∶1∶1,水相介质为蒸馏水,温度为50℃,搅拌速度为30 rpm。最佳处方制备的平均包封率为91.9%,Zeta电位为-32.1 mV,平均粒径为170.3 nm。结论:该实验制备的复方鸦胆子油脂质体具有包分率高、稳定性好、表面带负电等特点,为进一步研究复方鸦胆子油脂质体奠定了基础。

Objective ： To optimize the prescription and preparation of compound oleum fructus bruceae liposomes. Methods： The encapsulation efficiency of liposomes was examined by Gas Chromatography. Orthogonal design was adopted and encap- sulation efficiency of liposomes was taken as index in observation. Formulation and preparation factors which may influence properties of liposomes were studied. Result： Compound oleum fructus bruceae liposomes was prepared by ethanol injection method. The optimum preparation conditions were as follows：the concentration of the soybean lecithin was 1.5% ,ratio of lecithin to cholesterol was 5：1 ,volume ratio of water-oil was 10：1 ,the best proportion for mannitol,suerose,lecithin was 1：1：1, the aqueous phase was distilled water,the temperature was 50 ~C ,and the stirring speed was 30 rpm. The average encapsula- tion efficiency was 91.9%. The Zeta potential of the liposomes was -32.1 mV and the average size was 170.3 nm. Conclu- sion ：The formulation and preparation process were practical to prepare the compound liposomes with good encapsulation efficiency and stability, negative charged surface. It was valuable to be further study for oleum fructus brueeae liposomes.