Polymeric micelles for acyclovir drug delivery.
Polymeric micelles for acyclovir drug delivery.
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用于阿昔洛韦药物递送的聚合物胶束。
DOI：
10.1016/j.colsurfb.2014.08.011
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发表时间：
2014
期刊：
影响因子：
--
通讯作者：
Peng,Ching-An
中科院分区：
文献类型：
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作者：
Sawdon,AliciaJ;Peng,Ching-An
合成了阿昔洛韦(Acylovir，ACV)聚合物前药胶束。首先，以环氧氯丙烷为引发剂，引发ɛ-己内酯开环聚合，得到环己酮-聚己内酯(ACV-PCL)。通过将疏水性ACV-PCL与亲水性甲氧基聚乙二醇酯(Mpeg)或壳聚糖偶联，形成了可用于药物释放的聚合物胶束，通过1HNMR、FTIR和凝胶渗透色谱表征了mEg或壳聚糖与疏水性ACV-PCL的偶联。通过动态光散射、Zeta电位分析、透射电子显微镜和临界胶束浓度(CMC)等手段对合成的ACV标记聚合物胶束进行了表征。结果表明，聚合物胶束的平均粒径在200 nm以下，阿昔洛韦-聚乙二醇单甲醚和阿昔洛韦-壳聚糖在L−1和L−1的cmc分别为2.0 mg和6.6 mg。对阿昔洛韦的药物释放动力学进行了研究，细胞毒性实验表明，阿昔洛韦标记的聚合物胶束无毒。
Polymeric prodrug micelles for delivery of acyclovir (ACV) were synthesized. First, ACV was used directly to initiate ring-opening polymerization of ɛ-caprolactone to form ACV-polycaprolactone (ACV-PCL). Through conjugation of hydrophobic ACV-PCL with hydrophilic methoxy poly(ethylene glycol) (MPEG) or chitosan, polymeric micelles for drug delivery were formed.1H NMR, FTIR, and gel permeation chromatography were employed to show successful conjugation of MPEG or chitosan to hydrophobic ACV-PCL. Through dynamic light scattering, zeta potential analysis, transmission electron microscopy, and critical micelle concentration (CMC), the synthesized ACV-tagged polymeric micelles were characterized. It was found that the average size of the polymeric micelles was under 200 nm and the CMCs of ACV-PCL-MPEG and ACV-PCL-chitosan were 2.0 mg L−1and 6.6 mg L−1, respectively. The drug release kinetics of ACV was investigated and cytotoxicity assay demonstrates that ACV-tagged polymeric micelles were non-toxic.