Wang Wenlong, Chen Shu, Zhang Liang, Wu Xi, Wang Jiexin, Chen Jian-Feng, Le Yuan
State Key Laboratory of Organic-Inorganic Composites, Beijing University of Chemical Technology, Beijing 100029, PR China.
Department of Chemical Engineering, University College of London, Gower Street, London, England.
Mater Sci Eng C Mater Biol Appl. 2015 Jan;46:514-20. doi: 10.1016/j.msec.2014.10.048. Epub 2014 Oct 23.
Poly(lactic acid) (PLA) is a kind of non-toxic biological materials with excellent absorbability, biocompatibility and biodegradability, which can be used for drug release, tissue engineering and surgical treatment applications. In this study, we prepared chitosan modified PLA nanoparticles as carriers for encapsulation of docetaxel by anti-solvent precipitation method. The morphology, particle size, zeta potential and composition of the PLA/chitosan were characterized by SEM, DLS, FTIR and XPS. As-prepared PLA/chitosan particles exhibited average size of 250 nm and showed very narrow distribution with polydispersity index of 0.098. Their large surface charge-ability was confirmed by zeta potential value of 53.9 mV. Docetaxel was released from PLA/chitosan nanoparticles with 40% initial burst release in 5 h and 70% cumulative release within 24 h, while from PLA nanoparticles 65% of docetaxel was released in 5h. In vitro drug release study demonstrated that PLA/chitosan nanoparticles prolonged drug release and decreased the burst release over the unmodified PLA nanoparticles. These results illustrated high potential of chitosan modified PLA nanoparticles for usage as anticancer drug carriers.
聚乳酸（PLA）是一种无毒的生物材料，具有优异的吸收性、生物相容性和生物降解性，可用于药物释放、组织工程和外科治疗应用。在本研究中，我们通过反溶剂沉淀法制备了壳聚糖修饰的PLA纳米颗粒作为多西他赛的包封载体。通过扫描电子显微镜（SEM）、动态光散射（DLS）、傅里叶变换红外光谱（FTIR）和X射线光电子能谱（XPS）对PLA/壳聚糖的形态、粒径、zeta电位和组成进行了表征。所制备的PLA/壳聚糖颗粒的平均粒径为250nm，分散指数为0.098，显示出非常窄的粒径分布。zeta电位值为53.9mV证实了它们具有较大的表面带电能力。多西他赛从PLA/壳聚糖纳米颗粒中释放，在5小时内初始突释率为40%，24小时内累积释放率为70%，而从PLA纳米颗粒中5小时内多西他赛的释放率为65%。体外药物释放研究表明，与未修饰的PLA纳米颗粒相比，PLA/壳聚糖纳米颗粒延长了药物释放并降低了突释。这些结果表明壳聚糖修饰的PLA纳米颗粒作为抗癌药物载体具有很高的潜力。
