载紫杉醇-阿霉素微泡的制备以及控制释放研究  

Preparation and controlled-release characteristics of microbubbles loaded with paclitaxel and doxorubicin

作　　者：李露[1] 陈娟娟[1] 刘先俊[1] 

机构地区：[1]重庆医科大学基础医学院分子医学与肿瘤研究中心,重庆400016

出　　处：《第三军医大学学报》2012年第5期427-430,共4页Journal of Third Military Medical University

摘　　要：目的制备能同时携带2种抗肿瘤药物的脂质微泡,对其载药量以及体外控制释放能力进行研究。方法以机械振荡法制备脂质微泡,嵌入法对紫杉醇进行装载以及生物素-亲和素体系连接阿霉素脂质体。粒径分析仪以及荧光显微镜对其表征分析,紫外分光光度法以及酶标仪分别测定紫杉醇和阿霉素载药量;在超声辐照条件下,促使微泡对紫杉醇以及阿霉素的释放,并测定各自药物释放量确定超声辐照微泡的药物释放效率。结果粒径分析仪测得载药微泡其粒径约为(1.45±0.27)μm,荧光显微镜下能够观察到微泡周围显红色荧光;以3 mg固定磷脂用量,紫杉醇最大包封率为(54.64±2.98)%,每108个微泡载阿霉素量为(4.52±0.53)μg;当超声波机械指数为1.0时(MI=1.0),90%的微泡破碎以及紫杉醇和阿霉素释放率分别为15%和80%。结论载药微泡在超声辐照作用下具有良好的药物释放能力,能够在超声图像辅助给药体系为肿瘤治疗提供一种有效的双药载体。Objective To prepare ultrasound microbubbles（MBs） which can simultaneously load two anticancer drugs and investigate the drug-loading capacity and controlled-release characteristics.Methods MBs were fabricated by mechanical oscillation.Paclitaxel（PTX） was embedded into the membrane of MBs,and liposomes loaded with doxorubicin（DOX） were connected with MBs by biotin avidin linker system.The properties of prepared MBs were analyzed for their size by particle size analyzer and for their surface features by fluorescent microscopy.UV-visible spectrometry and multi-function microplate reader were used to identify their loaded doses of PTX and DOX respectively.The efficiency of ultrasound mediated drug release were identified by measuring the amount of PTX and DOX releasing from MBs.Results The prepared MBs were in an average diameter of（1.45±0.27） μm with red fluorescent surrounding.When 3 mg phospholipid was given,the maximum of PTX encapsulation efficiency was（54.64±2.98）% and each 1×108 microbubbles containing（4.52±0.53） μg DOX.When ultrasonic applications had the mechanical index of 1.0（MI=1.0）,the destruction of the MBs was 90% and the efficiency of PTX and DOX releasing were 15% and 80%,respectively.Conclusion Ultrasound radiation triggers drugs releasing from MBs,which might be used as an effective drug carrier that combining ultrasound image and drug delivery in the field of oncology treatment.

关 键 词：微泡 药物载体 紫杉醇 阿霉素 控制释放 

分 类 号：R943[医药卫生—药剂学] R944.9[医药卫生—药学]