Optimization of parameters for preparation of docetaxel-loaded PLGA nanoparticles by nanoprecipitation method
Optimization of parameters for preparation of docetaxel-loaded PLGA nanoparticles by nanoprecipitation method
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DOI：
10.1007/s11596-013-1192-x
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发表时间：
2013-10
期刊：
影响因子：
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通讯作者：
Wei Shi;Zhan-jie Zhang;Yin Yuan;En-ming Xing;Y. Qin;Zhen-jun Peng;Zhi-ping Zhang;Kun-yu Yang
中科院分区：
文献类型：
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作者：
Wei Shi;Zhan-jie Zhang;Yin Yuan;En-ming Xing;Y. Qin;Zhen-jun Peng;Zhi-ping Zhang;Kun-yu Yang
采用纳米沉淀法制备紫杉醇-聚（丙交酯-乙交酯）共聚物（PLGA）纳米粒，并优化相关工艺参数，以获得包封率高、粒径小的紫杉醇纳米粒。研究了纳米粒子的物理化学特性。最佳工艺条件为：油相为丙酮和乙醇的混合物，TPGS浓度为0.2%，油水比为1：5，理论药物浓度为5%。优化后的纳米粒子为球形，粒径在130 ~ 150 nm之间。包封率为（40.83±2.1）%。体外释放呈双相模式。结果表明，紫杉醇-PLGA纳米粒制备成功，有望作为多西他赛的新型载体，取代泰索帝，发挥更大的作用。
The purpose of this study was to develop docetaxel-poly (lactide-co-glycolide) (PLGA) loaded nanoparticles by using nanoprecipitation method and optimize the relative parameters to obtain nanoparticles with higher encapsulation efficiency and smaller size. The physicochemical characteristics of nanoparticles were studied. The optimized parameters were as follows: the oil phase was mixture of acetone and ethanol, concentration of tocopheryl polyethylene glycol succinate (TPGS) was 0.2%, the ratio of oil phase to water phase was 1:5, and the theoretical drug concentration was 5%. The optimized nanoparticles were spherical with size between 130 and 150 nm. The encapsulation efficiency was (40.83±2.1)%. Thein vitrorelease exhibited biphasic pattern. The results indicate that docetaxel-PLGA nanoparticles were successfully fabricated and may be used as the novel vehicles for docetaxel, which would replace Taxotere® and play great roles in future.