吲哚美辛聚氰基丙烯酸正丁酯纳米粒的制备

Preparation of indomethacin-polybutylcyanoacrylate nanoparticles

以生物降解型聚氰基丙烯酸正丁酯为载体材料,采用乳化聚合法制备吲哚美辛纳米粒,通过单因素试验初选、U5(53)均匀设计优选制备工艺,用透射显微镜、激光粒度分析仪、紫外分光光度法、X-射线衍射的手段对其特性进行了表征。结果表明,在pH 1.5,Dextran-70与Pluronic F-68质量比为4∶1,氰基丙烯酸正丁酯体积分数为0.7%,搅拌速度为800 r/min条件下制备的吲哚美辛纳米粒各项指标较为满意。特性研究表明:优化条件下制备的纳米粒球形圆整、无粘连、平均粒径为(127±3)nm,分布均匀,包封率为82.97%,载药量为64 mg/g,且吲哚美辛在纳米粒中的无定形程度增加。

Indomethacin-polybutylcyanoacrylate nanoparticles （IMC-PBCA） have been prepared using emulsion polymerization with biodegradable polybutylcyanoacrylate as a carrier material. The preparation procedure was optimized by single factor tests and uniform design with a Us （53） table. Dynamic laser light scattering, transmission electron microscopy, UV spectroscopy and XRD were used to characterize the nanoparticles. The results indicated that the optimum condition for the preparation of IMC-PBCA nanoparticles were pH 1.5, weight ratio of Dextran-70 to Pluronic F-68 4 ： 1, volume fraction of BCA 0.7 % and stirring speed 800 r/min. The nanoparticles were discrete and uniform spheres with average diameter （127 ± 3） nm and the encapsulation efficiency and drug loading of IMC-PBCA were 82.97 % and 64 mg/g, respectively. XRD indicated that the indomethacin in the nanoparticles was either dispersed in the polymer in an amorphous state or distributed in a crystalline state with the crystal size too small to be detected.