Box-Behnken效应面法优化制备主动靶向紫杉醇亚微乳及其体外抗肿瘤活性

发布时间：2018-06-04 01:03

本文选题：亚微乳 + 紫杉醇　；参考：《沈阳药科大学学报》2016年12期

【摘要】：目的采用Box-Behnken效应面法对紫杉醇亚微乳的处方进行优化从而制备具有稳定性良好的亚微乳。方法分别以中链油质量分数(X1)、磷脂质量分数(X2)、F68质量分数(X3)、油酸质量分数(X4)4个因素作为考察因素,以包封率和粒径为评价指标,采用4因素3水平Box-Behnken效应面设计法筛选SME/PTX的最优处方。采用透析法测定药物的体外释放行为,采用MTT法测定亚微乳对于肿瘤细胞的细胞毒性。结果最优处方工艺条件为X1=12.70,X2=1.95,X3=0.43,X4=0.05,根据最优处方制备的亚微乳的包封率和粒径与预测值存在较小的偏差,证明本方法可用于亚微乳的处方优化。在体外释放实验结果表明紫杉醇亚微乳具有明显的缓释行为。MTT实验结果表明紫杉醇亚微乳对MCF-7和Hep G2细胞的细胞毒性对比原料药组显著增强。结论Box-Behnken效应面法可用于优化制备紫杉醇亚微乳。
[Abstract]:Aim to optimize the formulation of paclitaxel microemulsion by Box-Behnken effect surface method. Methods four factors, I. e., middle chain oil mass fraction (X _ (1), phospholipid mass fraction (X _ (2) F _ (68) and oleic acid mass fraction (X _ (4) were used as test factors, and the entrapment efficiency and particle size were used as evaluation indexes. The optimal formulation of SME/PTX was selected by 4 factor 3 level Box-Behnken effect surface design method. The in vitro release behavior of the drug was determined by dialysis and the cytotoxicity of submicroemulsion to tumor cells was determined by MTT assay. Results the optimum conditions of formulation were X1X 12.70 X _ 2X _ 2H _ (1.95) X _ (3) C _ (3) C _ (0.4) X _ (4) O _ (0.05). There was a small deviation between the encapsulation efficiency and particle size and the predicted value according to the optimum formulation. It was proved that this method could be used to optimize the formulation of sub-microemulsion. The results of in vitro release test showed that paclitaxel submicron emulsion had obvious slow-release behavior. The results showed that the cytotoxicity of paclitaxel submicron emulsion to MCF-7 and Hep G2 cells was significantly increased compared with that of raw drug group. Conclusion Box-Behnken effect surface method can be used to optimize the preparation of paclitaxel submicron emulsion.
【作者单位】：沈阳医学院附属中心医院干部保健科;牡丹江医院附属红旗医院肿瘤科;沈阳药科大学药学院;沈阳医学院附属中心医院药剂科;
【基金】：沈阳市科技计划项目(F15-139-9-06;F15-199-1-24)
【分类号】：R943;R96

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