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出 处:《中国药师》2011年第3期303-307,共5页China Pharmacist
基 金:广东省科技计划项目(编号:2007B031404013)
摘 要: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 optimize the formulation and preparation technique of lung targeting ehitosan microspheres containing doeetaxel(DTX). Method: Chitosan was used to prepare the microspheres loading with docetaxel by emulsion chemical crosslinking method. The formulation and preparation technique were optimized by orthogonal experiment accorded to the results of single-factor selecting experiment. The drug-loading rate and drug yield were determined by HPLC. Result: The docetaxel chitosan microspheres were regular and smooth in their morphology observed under a microscope. The average particle size was ( 8. 63 ±0. 27 ) μm with 83.5% particles in the range of 7-12 μm. The drug-loading rate and drug yield were (25. 01 ±1.80)% and (85. 54 ±2. 21 )%, respectively. Conclusion: The docetaxel chitosan microspheres prepared by the optimized preparation technique are promising. The particle size is suitable for lung targeting. These microspheres could be a promising formulation for lung cancer therapy.
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