论文部分内容阅读
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。
OBJECTIVE To optimize the screening method for prescription of poly (ethylene glycol) methoxy-poly (D, L-lactide-co- lactide) mPEG-PDLLA) micelles. Methods The drug-loaded micelles of mPEG-PDLLA were prepared by thin-film dispersion method. The effects of film formation temperature (X1), hydration temperature (X2) and dosage (X3) The encapsulation efficiency (Y1, EE%), drug loading (Y2, wLC%), encapsulation efficiency of resveratrol (RES) ) As the evaluation index. The drug-loaded micellar prescription was screened by Box-Behnken design with 3-factor-3 level. The particle size and zeta potential of drug-loaded micelles were determined. Results The micellar entrapment efficiencies of the two copolymers were both higher than 98% and the drug loadings were both higher than 16%. The mean diameter of drug-loaded micelles was (17 ± 3.2) nm; the zeta potential was -18.0 mV. Conclusion The mathematical model optimized by Box-Behnken experimental design method has good predictability and can be used to optimize the formulation of docetaxel / resveratrol-loaded micelles.