Shi Wei, Zhang Zhan-Jie, Yuan Yin, Xing En-Ming, Qin You, Peng Zhen-Jun, Zhang Zhi-Ping, Yang Kun-Yu
Cancer Center, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China.
School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030, China.
J Huazhong Univ Sci Technolog Med Sci. 2013 Oct;33(5):754-758. doi: 10.1007/s11596-013-1192-x. Epub 2013 Oct 20.
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)%. The in vitro release 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.
本研究的目的是采用纳米沉淀法制备多西他赛-聚(丙交酯-乙交酯)(PLGA)纳米粒,并优化相关参数以获得具有更高包封率和更小粒径的纳米粒。研究了纳米粒的理化特性。优化后的参数如下:油相为丙酮和乙醇的混合物,聚乙二醇琥珀酸维生素E酯(TPGS)浓度为0.2%,油相与水相的比例为1:5,理论药物浓度为5%。优化后的纳米粒呈球形,粒径在130至150nm之间。包封率为(40.83±2.1)%。体外释放呈现双相模式。结果表明,多西他赛-PLGA纳米粒已成功制备,可作为多西他赛的新型载体,有望取代泰索帝®并在未来发挥重要作用。