【摘要】 目的通过优化手段筛选处方,制备同时包载多烯紫杉醇/白藜芦醇的单甲氧基聚乙二醇-聚丙交酯嵌段共聚物(poly(ethylene glycol)methoxy-poly(D,L-lactide)mPEG-PDLLA)胶束。方法采用薄膜分散法制备mPEG-PDLLA载药胶束,分别以成膜温度(X1)﹑水化温度(X2)、投药量(X3)为考察指标,以多烯他赛(docetaxel,DTX)的包封率(Y1,EE%)及载药质量分数(Y2,wLC%)、白藜芦醇(resveratrol,RES)的包封率(Y3,EE%)及载药质量分数(Y4,wLC%)为评价指标;采用3因素3水平Box-Behnken效应面设计法筛选载药胶束处方;并测定载药胶束的粒径和zeta电位。结果共聚物对2种药物的胶束包封率均大于98%,载药质量分数均大于16%。载药胶束的平均粒径为(17±3.2)nm;zeta电位为-18.0mV。结论采用Box-Behnken实验设计法优化处方所得到的数学模型预测性良好,可以用于多烯紫杉醇∕白藜芦醇载药胶束的处方优化。更多还原

【Abstract】 Objective To optimize the formulation of monomethoxy-poly(ethylene glycol)-b-poly(D,L-lactide)(mPEG-PDLLA)micelles containing docetaxel and resveratrol micelles.Methods Drugs loaded micelles were prepared by the membrane hydration method.A three factor,three-level BoxBehnken design was used for the optimization procedure with film forming temperature(X1),hydration temperature(X2),drug dosage(X3)as the independent variables and the entrapment efficiency of docetaxel(Y1),the loading content of docetaxel(Y2),the entrapment efficiency of resveratrol(Y3),the loading content of resveratrol(Y4)as the response variable.The particle size distribution and zeta potential of the drug loaded micelles were determined.Results The optimized micelles showed entrapment efficiency more than98% and drug loaded content more than16%.The particle size of the dual drug loaded micelles was(17±3.2)nm,with zeta potential of-18.0 mV.Conclusions The formation of dual drug loaded micelles could be optimized by the Box-Behnken design.更多还原