喜树碱衍生物CZ48缓释纳米粒的制备及其体外释药特性考察

目的:制备喜树碱衍生物CZ48缓释纳米粒并考察其体外释药特性。方法:以聚乳酸(PLA)为材料,采用W/O/W型乳化溶剂挥发法制备CZ48缓释纳米粒,通过透射电子显微镜观察纳米粒的微观形态,采用粒度分析仪测定粒径并考察该制剂的体外释药特性。结果:CZ48缓释纳米粒呈明显的球状结构,粒度(260.6±3.2)nm,载药量(11.8±1.29)%,包封率(88.7±2.55)%,体外释放可持续48 h,累积释放率达85%。结论:制备的CZ48缓释纳米粒包封率和载药量高,缓释效果明显,为该制剂的药代动力学研究提供数据支持。

Preparation and in vitro Release of CZ48 Sustained-release Nanoparticles

Objective: To prepare CZ48 sustained-release nanoparticles and investigate its in vitro release. Method: Using polylactic acid(PLA) as material,CZ48 sustained-release nanoparticles was prepared through W/O/W double emulsion technique,its micromorphology was observed by transmission electron microscope,particle size was determined by particle size analyzer and in vitro release was investigated. Result: CZ48 sustained-release nanoparticles showed obvious spherical structure with particle size of (260.6±3.2)nm,encapsulation efficiency of (88.7±2.55)% and drug-loading of (11.8±1.29)%,in vitro release studies showed that 85% of CZ48 was released from sustained-release nanoparticles in the first 48 h. Conclusion: These prepared CZ48 sustained-release nanoparticles are successfully prepared through W/O/W double emulsion technique with satisfactory encapsulation efficiency and drug-loading and obvious sustained-release,which provides data support for further research on pharmacokinetic.