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首页> 外文期刊>Journal of Applied Polymer Science >In vitro evaluation of efficacy of dihydroartemisinin-loaded methoxy poly(ethylene glycol)/poly(L-lactic acid) amphiphilic block copolymeric micelles
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In vitro evaluation of efficacy of dihydroartemisinin-loaded methoxy poly(ethylene glycol)/poly(L-lactic acid) amphiphilic block copolymeric micelles

机译：载有双氢青蒿素的甲氧基聚（乙二醇）/聚（L-乳酸）两亲嵌段共聚物胶束的体外评价

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摘要

Dihydroartemisinin (DHA)-loaded methoxy poly(ethylene glycol)/poly(l-lactic acid) (mPEG_(5000)-PLLA_(3200)) amphiphilic block copolymeric micelles (DHA-CM) have been prepared using modified solvent evaporation method. Physicochemical properties of DHA-CM were investigated by using dynamic light scattering, transmission electron microscopy, high-performance liquid chromatography, and Fourier transform infrared. Polymers formed stable, spherical, and worm-like micelles with mean sizes smaller than 130 nm. In vitro release experiments revealed that DHA-CM provided a more solubilizing effect than DHA suspension; in addition, it was showed that drug release profiles highly depended on pH values of dissolution media. Various types of lyoprotectants were tested to improve the redispersion performance of the freeze-dried products. 3-(4, 5-dimethyl- thiazol-2-yl)-2, 5-diphenyl tetrazolium bromide assay was used to evaluate the cytotoxicity of micellar solutions of freeze-dried DHA-CM. The results showed that the IC_(50) values of DHA-CM and DHA suspension for KB cell lines were 18.70 and 24.55 μM, respectively. However, DHA-CM had little cytotoxicity for L02 cell lines.
机译：已使用改进的溶剂蒸发方法制备了负载二氢青蒿素（DHA）的甲氧基聚（乙二醇）/聚（l-乳酸）（mPEG_（5000）-PLLA_（3200））两亲嵌段共聚物胶束（DHA-CM）。通过动态光散射，透射电子显微镜，高效液相色谱和傅里叶变换红外光谱研究了DHA-CM的理化性质。聚合物形成稳定，球形和蠕虫状的胶束，平均尺寸小于130 nm。体外释放实验表明，DHA-CM比DHA悬浮液具有更好的增溶作用。此外，已表明药物释放曲线高度依赖于溶出介质的pH值。测试了各种类型的冻干保护剂以改善冷冻干燥产品的再分散性能。使用3-（4,5-二甲基-噻唑-2-基）-2,5-二苯基溴化四氮唑测定法评估冻干DHA-CM的胶束溶液的细胞毒性。结果表明，KB细胞系DHA-CM和DHA悬浮液的IC_（50）值分别为18.70和24.55μM。但是，DHA-CM对L02细胞株几乎没有细胞毒性。

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