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

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。

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.