TechnicalOptimizationofPreparationofHCPTloadedPLGAMicrovesiclesbyUltrasound.docVIP

10-羟喜树碱PLGA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） 10-羟基喜树碱（camptothecin，HCPT）25mg，乳酸-羟基乙酸共聚物[poly(1actic-co-glycolic acid)，PLGA] 1.875g，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-40～0mv为主，粒径500～1000nm，包封率为80.99%，载药量为0.6972%，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 Technical Optimization of Preparation of HCPT-loaded PLGA Microvesicles by Ultrasound WU Qing，ZHU Zhao-jing（School of Pharmacy, Chonging University of Medical Sciences, Chongqing 400016，China） Objective To discuss the efects of technical conditions on the microvesicles size , envelopment rate,morphology of surface and so on to choose the best technical condition to prepare HCPT-loaded PLGA microvesicles for injection guided by ultrasound．Methods Micro were prepared by a water/oil/water emulsion and solvent evaporation method．Various factors related with the envelopment and micmparticle size were studied．The experimental design was chosen to optimize the technology of microvesicles preparation．Result best processing conditions for preparing microvesicles were as following ： PLGA 1.875g, the PVA concentration was2%,the ratio of intemal and external phases was 1:5.These preparative variables can prepare global, smooth and glossy microvesicles.Electric charges were probably between －40-0mv, microvesicles sizes were probably between500-1000nm，envelopment rate was 80.99% ,drug loading of the microvesicles was 0.6972%，and ultrasonic imaging was clear in vitro. Conclusion Optimize technical condition can prepare injectablemicrovesicles by ultrasound. Key words: camptothecin；poly(1actic-co-glycolic acid)；microvesicles；preparation；optimization 随着超声影像技术的不断发展和超声微泡制备技术的不断改进，具有可视、靶向性的超声微泡在对组织、血栓及肿瘤的诊断与治疗中发挥了重要作用。10-羟基喜树碱（camptothecin，HCPT）来自喜树（camptotheca acuminata）皮、果实，是DNA拓扑异构酶Ⅰ(TOPO-Ⅰ)抑制剂[1]，目前也有半合成衍生物。其抗肿瘤活性强、抗瘤谱广、毒性较低，且与其他常用抗肿瘤药无交叉耐药性，广泛应用于肝癌、胃癌、头颈部癌症及白血病等多种恶性肿瘤的治疗。虽然是较有发展前景的抗癌药物，但其特殊的理化性质使得临床应用受到限制[2]，例如临床使用的经碱化开环后溶于水的注射液会