穿膜肽修饰表阿霉素与五味子乙素脂质体的处方优选及细胞毒性评价

Formulation Optimization and Cytotoxicity Evaluation of PFV Modified Epirubicin and Schisandrin B Liposomes

目的构建穿膜肽修饰表阿霉素与五味子乙素脂质体,通过正交试验设计优选出最佳制备工艺,并对构建的脂质体进行细胞毒性评价。方法采用硫酸铵梯度法制备脂质体,采用高效液相色谱仪测定脂质体包封率,利用正交设计优选出脂质体的最佳制备工艺,最后采用SRB染色法进行细胞毒性实验以考察脂质体对肿瘤细胞的杀伤效果。结果脂质体的最优处方为磷脂:胆固醇=5∶1(质量比),磷脂:表阿霉素=25∶1(质量比),水化环境pH=7.3,细胞粉碎功率为500 W。穿膜肽修饰表阿霉素与五味子乙素脂质体对LLT细胞的IC50值为(2.65±1.57)μmol/L,对U87细胞的IC50值为(4.96±3.46)μmol/L。结论优选出的穿膜肽修饰表阿霉素与五味子乙素脂质体的制备工艺条件的重复性良好,操作简便,构建的脂质体具有明显的肿瘤细胞毒性。

Objective:PFV modified epirubicin plus schisandrinB liposomes were prepared,the best prescription was optimized by orthogonal design and the cytotoxic effects were evaluated.Method:Liposomes were constructed by ammonium sulfate gradient method,the experimental group was designed by using the orthogonal design and the encapsulation rate of liposomes was determined by HPLC.The cytotoxicity of liposomes to cancer cells was studied by SRB staining.Results:The optimal prescription of liposomes was phospholipid:cholesterol=5∶1(mass ratio),phospholipid:epirubicin=25∶1(mass ratio),the pH of hydration environment was 7.3,the ultrasonic crushing power was 500 W.The IC50 value of liposomes for LLT cells was(2.65±1.57)μmol/L,and(4.96±3.46)μmol/L for U87 cells,respectively.Conclusion:The preparation process optimized by orthogonal design had a good repeatability and simple preparation,the optimal liposomes were more cytotoxic than the ordinary liposomes.