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目的:研制肺靶向多西紫杉醇壳聚糖微球,并对处方工艺进行筛选。方法:以壳聚糖为载体,采用乳化-化学交联法制备多西紫杉醇壳聚糖微球。在单因素考察的基础上,利用正交试验设计优化微球制备工艺,采用HPLC法测定微球的载药量与包封产率。结果:制得的微球显微观察形态圆整、表面光滑,无粘连;平均粒径为(8.63±0.27)μm,粒径7～12μm的微球平均占总数的83.5%,载药量为(25.01±1.80)%,包封产率为(85.54±2.21)%。结论:筛选的最佳处方工艺制备的微球粒径大小适宜,可满足肺靶向微球的要求;该制剂有可能成为,临床肺部肿瘤治疗的一种靶向制剂。
Objective: To develop lung-targeting docetaxel chitosan microspheres and to screen the prescription process. Methods: The docetaxel chitosan microspheres were prepared by emulsion-chemical cross-linking method using chitosan as carrier. On the basis of single-factor investigation, the orthogonal design was used to optimize the preparation process of microspheres. The drug loading and encapsulation efficiency of microspheres were determined by HPLC. Results: The microspheres microspheres were round and smooth in shape with no adhesion. The mean diameter of the microspheres was (8.63 ± 0.27) μm and the diameter of the microspheres with the diameter of 7 ~ 12 μm was 83.5% (25.01 ± 1.80)%, the encapsulation yield was (85.54 ± 2.21)%. CONCLUSIONS: The particle size of microspheres prepared by the best prescription process is suitable to meet the requirements of lung-targeting microspheres. The preparation may become a targeted agent for the treatment of clinical lung tumors.