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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 (MXFX-PBCA-NP) and test its quality. Methods: MXFX-PBCA-NP was prepared by emulsion polymerization. The preparation process of MXFX-PBCA-NP was optimized by single factor test. The drug loading, entrapment efficiency and cumulative drug release curve were determined by HPLC. The average particle size, atomic force microscope observation of the morphology of nanoparticles. Results: MXFX-PBCA-NP was slightly spherical with the average size of 89.5nm. The average drug loading was 11.7% and the entrapment efficiency was 89.2%. There was no significant change in drug loading and particle size of MXFX-PBCA-NP in vitro 2h cumulative release of 33.5%, 60h cumulative release of 81.3%. Conclusion: The freeze-dried powder of MXFX-PBCA-NP prepared by emulsion polymerization has good stability and dual characteristics of burst release and sustained release.