载莫西沙星聚乳酸-羟基乙酸缓释微球的制备与体外释放研究

Preparation and in vitro release research of moxifloxacin-loaded polylactic acidglycolic acid sustained-release microspheres

目的 制备用于治疗脊柱结核的载莫西沙星聚乳酸-羟基乙酸（PLGA）缓释微球,观察其体外理化特性和缓释性能。方法 以PLGA为药物载体,采用优化O/W乳化-溶剂挥发法制备载莫西沙星-PLGA缓释微球,用光学显微镜和扫描电子显微镜观察微球的形态特征。采用超声破碎法震碎微球,然后检测莫西沙星-PLGA缓释微球的载药率和包封率。采用恒温振荡法观察药物的体外释放规律。结果 光学显微镜下观察莫西沙星-PLGA缓释微球成圆形,表面光滑,分散均匀。扫描电子显微镜下观察缓释微球成球良好,颗粒规整,大小均匀,微球间无粘连,微球聚集不明显且表面分布有较均匀的微孔。莫西沙星-PLGA缓释微球粒径为12～20（15.6±4.3）μm,载药率为（21.5±0.31）%,包封率为（77.4±1.6）%。莫西沙星-PLGA缓释微球的体外药物释放过程较为平稳,前14 d为突释期,突释期内累计释放率为55.3%,到50 d时体外累积释放率为92.3%。结论 制备的载莫西沙星-PLGA缓释微球形态良好、大小均匀且体外释放性能良好。

Objective To produce moxifloxacin-loaded polylactic acid-glycolic acid(PLGA) sustained release microspheres for treatment of spinal tuberculosis, and observe its physical and chemical properties and release characteristics in vitro.Methods The moxifloxacin-loaded sustained-release microspheres were prepared by optimized O/W emulsification-solvent evaporation method using PLGA as the drug carrier. The morphological characteristics of the microspheres were observed by optical microscope and scanning electron microscope. The microspheres were shredded by ultrasonication, and then the drug loading rate and encapsulation efficiency of moxifloxacin-loaded PLGA sustained-release microspheres were monitored. The pattern of drug release in vitro was observed by using constant temperature oscillation method. Results Under the optical microscope, the moxifloxacin-PLGA sustained-release microspheres had a round shape with smooth surface and uniform dispersion. Under the scanning electron microscope, the microspheres were well formed, the particles were regular, and the size was uniform; there was no adhesion between the microspheres, the microspheres were not concentrated, and the surface was distributed with uniform micropores. The particle size of moxifloxacin-PLGA sustained-release microspheres was 12-20(15.6±4.3) μm, the drug loading rate was(21.5±0.31)%, and the encapsulation efficiency was(77.4±1.6)%. The drug release profile of moxifloxacin-PLGA sustained-release microspheres in vitro was smooth and the sustained-release process was relatively stable. The first 14 days were the burst release period, the cumulative release rate during the burst release period was 55.3%, and the cumulative release rate in vitro was 92.3% at 50 days. Conclusion The shape of moxifloxacin-PLGA sustained release microsphere is regular, size is similar and release property in vitro is good.