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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。
OBJECTIVE: To prepare camptothecin derivative CZ48 sustained release nanoparticles and study its in vitro release characteristics. Methods: Polylactic acid (PLA) was used as material to prepare CZ48 sustained-release nanoparticles by W / O / W emulsion solvent evaporation method. The microscopic morphology of nanoparticles was observed by transmission electron microscopy. The particle size was measured by particle size analyzer. Preparation in vitro release characteristics. Results: The CZ48 sustained-release nanoparticles showed a spherical structure with a particle size of (260.6 ± 3.2) nm, drug loading (11.8 ± 1.29)% and entrapment efficiency of 88.7 ± 2.55% Rate of 85%. CONCLUSION: The prepared CZ48 sustained-release nanoparticles have high entrapment efficiency and sustained drug release rate and provide data support for the pharmacokinetics of the preparation.