10-羟基喜树碱乳酸-羟基乙酸共聚物超声微泡制备及工艺优化.docVIP

10-羟基喜树碱乳酸-羟基乙酸共聚物超声微泡制备及工艺优化 吴 青，朱照静（重庆医科大学药学院药剂学教研室，重庆 400016） 摘 要： 目的 探讨超声微泡的制备条件对粒径、包封率、表面形态等的影响，确定制备超声微泡的最佳工艺条件。 方法 以W/O/W型乳化溶剂挥发法制备微球，采用单因素实验和正交设计实验优化制备工艺。 结果 制备超声微泡的最佳条件是10-羟基喜树碱(10-hydroxy-camptothecin, HCPT) 25 mg，乳酸-羟基乙酸共聚物[poly(1actic-co-glycolic acid)，PLGA] 1.875 g，聚乙烯醇（PVA）浓度2%，内、外水相体积比为1∶5；此条件所制备超声微泡呈规则球形，表面光滑，电荷以-40～0 mv为主，粒径500～1 000 nm，包封率为80.99%，载药量为0.697 2%，体外超声成像清楚。 结论 优化制备条件，可制备出符合注射要求的超声微泡。 关键词：10-羟基喜树碱；乳酸-羟基乙酸共聚物；超声微泡；制备；优化 中图法分类号： 文献标识码：A Preparation and process optimization of HCPT-loaded PLGA microvesicles by ultrasound WU Qing, ZHU Zhao-jing (Department of Pharmaceutics, School of Pharmacy, Chongqing Medical University, Chongqing 400016, China) Abstract: Objective To investigate the effects of different technical conditions on the microvesicle size, envelopment rate, morphology of surface and so on in order to select the best technical conditions to prepare HCPT(10-hydroxy-camptothecin)-loaded PLGA microvesicles．Methods Microvesicles were prepared by a water/oil/water emulsion and solvent evaporation method．Various factors related the envelopment rate and micmparticle size were studied, such as the ratio of water phase and oil phase, ultrasound power, and time, stirring time and so on. Single facter experiments and orthogonal design testing was carried out to optimize the technology of microvesicles preparation．Results The best processing conditions for microvesicles prepar were as following: HCPT 25 mg, PLGA 1.875 g, the PVA concentration 2%, and the ratio of intemal and external phases 1:5. These preparative variables produced global, smooth and glossy microvesicles. Electric charges were probably between －400 mV, microvesicles sizes ranged from 500 to 1 000 nm, envelopment rate was 80.99%, drug loading to the microvesicles was 0.6972%, and ultrasonic imaging was clear in vitro. Conclusion Our optimize technical conditions can prepare injectable microvesicles by ultrasound. Key words: camptot