Guo Fangyuan, Guo Dingjia, Zhang Wei, Yan Qinying, Yang Yan, Hong Weiyong, Yang Gensheng
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, China.
College of Mechanical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.
Eur J Pharm Sci. 2017 Mar 1;99:328-336. doi: 10.1016/j.ejps.2017.01.001. Epub 2017 Jan 3.
Biodegradable polymeric nanoparticles (NPs) have potential therapeutic applications; however, preparing NPs of a specific diameter and uniform size distribution is a challenge. In this work, we fabricated a microchannel system for the preparation of curcumin (Cur)-loaded NPs by the interfacial precipitation method, which rapidly and consistently generated stable NPs with a relatively smaller diameter, narrow size distribution, and higher drug-loading capacity and entrapment efficiency. Poly(ε-caprolactone)-poly(ethylene glycol)-poly (ε-caprolactone) triblock copolymers(PCEC) used as the carrier material was synthesized and characterized. Cur-loaded PCEC NPs had an average size of 167.2nm with a zeta potential of -29.23mV, and showed a loading capacity and drug entrapment efficiency of 15.28%±0.23% and 96.11%±0.13%, respectively. Meanwhile, the NPs demonstrated good biocompatibility and bioavailability, efficient cellular uptake, and long circulation time and a possible liver targeting effect in vivo. These results indicate that the Cur-loaded PCEC NPs can be used as drug carriers in controlled delivery systems and other biomedical applications.
可生物降解的聚合物纳米颗粒（NPs）具有潜在的治疗应用；然而，制备具有特定直径和均匀尺寸分布的纳米颗粒是一项挑战。在这项工作中，我们构建了一个微通道系统，用于通过界面沉淀法制备载有姜黄素（Cur）的纳米颗粒，该方法能快速且持续地生成稳定的纳米颗粒，其直径相对较小、尺寸分布窄、载药量高且包封率高。合成并表征了用作载体材料的聚（ε-己内酯）-聚（乙二醇）-聚（ε-己内酯）三嵌段共聚物（PCEC）。载有Cur的PCEC纳米颗粒的平均尺寸为167.2nm，zeta电位为-29.23mV，载药量和药物包封率分别为15.28%±0.23%和96.11%±0.13%。同时，这些纳米颗粒表现出良好的生物相容性和生物利用度、高效的细胞摄取、较长的循环时间以及体内可能的肝靶向作用。这些结果表明，载有Cur的PCEC纳米颗粒可作为控释系统及其他生物医学应用中的药物载体。
