紫杉醇和多西紫杉醇双药胶束体外稳定性考察
In vitro stability of paclitaxel and docetaxel binary-drug loaded micelles
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摘要: 对紫杉醇和多西紫杉醇双药胶束稳定性进行了研究。用聚乙二醇单甲醚-聚乳酸嵌段共聚物(mPEG-PLA)同时增溶紫杉醇和多西紫杉醇，并对比考察体外稳定性的变化。当药物质量浓度为1 mg/mL、载药率为10%时，紫杉醇和多西紫杉醇单药胶束(single-drug loaded micelles，SDM)分别在9 h和1 h内稳定；当两种药物的载药率都为25%时，双药胶束(binary-drug loaded micelles，BDM)稳定性能超过24 h。此外，双药胶束在高浓度(≥1 mg/mL)时比低浓度(0.04 mg/mL)更加稳定。双药胶束用透射电镜观察，发现了一种网状结构。体外药物释放实验表明，双药胶束的释药速度比单药胶束快。双药胶束作为一种高载药率和高稳定性的载药形式，是胶束设计的一个新的选择。Abstract: The binary-drug loaded micelles(BDM)，in which paclitaxel(PTX) and docetaxel(DTX) co-solubilized with the monomethoxy poly(ethylene glycol)-block-poly(D，L-lactide)(mPEG-PLA) copolymer，were prepared and evaluated for their in vitro stability.It was found that the stabilities of paclitaxel and docetaxel single-drug loaded micelles(SDM) with a drug-loading content of 10% maintained in the period of 9 h and 1 h,respectively，whereas the stable period of BDM with both drug-loading content of 25% was up to 24 h.Moreover，the BDM showed better physical stability at high drug concentration(≥1 mg/mL) than low concentration(0.04 mg/mL).In addition,a network structure of the BDM was observed using transmission electron microscopy(TEM).Faster in vitro release of paclitaxel and/or docetaxel from the BDM was found if compared with those of SDM.BDM in the potentials such as high drug-loading content and excellent stability might be an alternative to the micelles design.
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