星点设计-响应面法优化穿膜肽修饰紫杉醇和他莫昔芬脂质体的处方

Optimizing Prescription of CPP Modified Paclitaxel plus Tamoxifen Liposomes by Central Composite Design-Response Surface Method

目的:采用响应面法优选出制备穿膜肽(CPP)修饰紫杉醇和他莫昔芬脂质体的最佳处方。方法:采用薄膜分散-硫酸铵梯度法制备CPP修饰紫杉醇和他莫昔芬脂质体,以磷脂/胆固醇(摩尔比),磷脂/聚乙二醇-二硬脂酰磷脂酰乙醇胺(摩尔比),磷脂/紫杉醇(摩尔比)为自变量,以修饰紫杉醇和他莫昔芬包封率的综合评分为因变量进行二次多项拟合。结果:脂质体的最优处方为磷脂/胆固醇=50:1,磷脂/PEG 2000-DSPE=5.5:1,磷脂/紫杉醇=50:1,脂质体中紫杉醇和他莫昔芬含量的综合评分为95.48%。结论:星点设计-响应面法优选出了CPP修饰紫杉醇和他莫昔芬脂质体的最佳处方。

Objective：To optimize the prescription of CPP modified paclitaxel plus tamoxifen liposomes by central composite design - response surface methodology. Methods ： The CPP modified paelitaxel plus tamoxifen liposomes was prepared by film dis- persion - ammonium sulfate gradient method. The mole ratios of EPC/CHOL, EPC/PEG2000 - DSPE and EPC/paclitaxel were used as the independent variable, and the encapsulation efficiencies of paclitaxel and tamoxifen were used as the dependent varia- ble. Results：The final optimal prescription of the liposomes was EPC/CHOL = 50： 1, EPC/PEG2000 -DSPE = 5.5：1 and EPC/ paclitaxel = 50：1. The encapsulation efficiencies of the paclitaxel and tamoxifen were 95.48%. Conclusion：Central composite de- sign - response surface methodology can optimize the optimal formulation of CPP modified paclitaxel plus tamoxifen liposomes.