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(lactic-co-glycolic acid),PLGA]1.875 g,初乳和外水相体积比为1∶15,聚乙烯醇(PVA)浓度3%;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,粒径为500～1 000 nm,包封率为79.33%,载药量为0.478 3%,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。
Objective To investigate the effects of different technical envelopment rate, morphology of surface and so on in order to select the HCPT（10-hydroxy-camptothecin）-loaded PLGA microvesicles. Methods conditions on the microvesicle size, best technical conditions to prepare Microvesicles were prepared by a water/oil/water emulsion and solvent evaporation method. Various factors related to 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 factor experiments and orthogonal design testing was carried out to optimize the technology of microvesicles preparation. Results The best processing conditions for microvesicles preparation were as following ： HCPT 25 mg, PLGA 1. 875 g, the ratio of internal and external phases 1 ： 15, and the PVA concentration 3%. These preparative variables produced global, smooth and glossy microvesicles. Electric charges were probably between -40 to 0 mV, microvesicles sizes ranged from 500 to 1 000 nm, envelopment rate was 79.33%, drug loading to the microvesicles was 0. 478 3%, and ultrasonic imaging was clear in vitro. Conclusion Our optimize technical conditions can prepare injectable microvesicles by ultrasound.
出处
《第三军医大学学报》
CAS
CSCD
北大核心
2009年第14期1349-1352,共4页
Journal of Third Military Medical University
