莫西沙星聚氰基丙烯酸正丁酯纳米粒的性质及制备优化

Preparation and in vitro release of moxifloxacin polybutylcyanoacrylate nanoparticles

目的:制备莫西沙星聚氰基丙烯酸正丁酯纳米粒(MXFX-PBCA-NP),并对其质量进行检测。方法:采用乳化聚合法制备MXFX-PBCA-NP,单因素试验法优化MXFX-PBCA-NP的制备工艺,高效液相法测定载药量、包封率及体外累积释药曲线,激光粒度仪测定平均粒径,原子力显微镜观察纳米粒的形态。结果:MXFX-PBCA-NP略呈球形,大小均匀,平均粒径89.5nm,平均载药量11.7%、包封率89.2%,样品保存6个月载药量及粒径均无明显变化,体外2h累积释药量33.5%,60h时累积释药量81.3%。结论:采用乳化聚合法制备的MXFX-PBCA-NP冻干粉稳定性好,并具有突释和缓释的双重特征。

OBJECTIVE To prepare moxifloxacin polybutylcyanoacrylate nanoparticles with high drug loading rate and evaluate its quality. METHODS Preparation of MXFX-PBCA-NP was performed by the Emulsion Polymerization with single-factor test optimization of Process,Drug loading, encapsulation efficiency and in vitro release cumulative curve were determine, laser particle size analyzer was used for testing the average particle size, atomic force microscopy for observation of nanoparticles pat terns. RESULTS The MXFX-PBCA-NP was slightly spherical, uniform size with the average size of 89. 5 nm, the average drug loading of 11. 7%, encapsulation efficiency of 89. 2%, there was no significant change in drug loading and size after stored for 6 minth, in vitro 2 h cumulative release was 33. 5%, 60 h cumulative release was 81.3 %. CONCLUSION MXFX-PBCA- NP prepored by the Emulsion Polymerization is stable with burst release and slow-release characteristics.