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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 formulation of paclitaxel and tamoxifen liposomes for preparation of penetrating peptide (CPP) by response surface methodology. Methods: CPP-modified paclitaxel and tamoxifen liposomes were prepared by the membrane dispersion-ammonium sulfate gradient method. The phospholipid / cholesterol (molar ratio), phospholipid / polyethylene glycol- distearoylphosphatidylethanolamine (molar ratio) , Phospholipid / paclitaxel (molar ratio) as independent variables, modified paclitaxel and tamoxifen encapsulation efficiency of the composite score as the second variable multiple fit. RESULTS: The optimal formulation of liposomes was phospholipid / cholesterol = 50: 1, phospholipid / PEG 2000-DSPE = 5.5: 1, phospholipid / paclitaxel = 50: 1, and the combination of paclitaxel and tamoxifen in liposomes The score is 95.48%. CONCLUSIONS: The best prescription of CPP-modified paclitaxel and tamoxifen liposomes is optimized by the star-point design-response surface method.