载紫杉醇-阿霉素微泡的制备以及控制释放研究.docVIP

(载紫杉醇-阿霉素微泡的制备以及控制释放研究 李露，陈娟娟，刘先俊（400016 重庆，重庆医科大学基础医学院分子医学与肿瘤研究中心） [] 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；并在不同超声辐照条件下，通过测定游离药物浓度对其药物释放效率进行评价。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3mg固定磷脂用量，紫杉醇最大包封率为（54.64±2.98）%，每108微泡载阿霉素量为（4.52±0.53）μg；当MI=1.0，微泡破碎率达90%，阿霉素释放释放率约为80%，紫杉醇释放率接近15%。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。 [关键词] 微泡；药物载体；紫杉醇；阿霉素；控制释放 [中图法分类号] [文献标志码] A Preparation and controlled-release characteristics of microbubbles loaded with paclitaxel and doxorubicin Li Lu,Chen Juanjuan,Liu Xianjun（1Molecular Medicine and Cancer Research Center, College of Basic Medicine, Chongqing Medical University ,Chongqing, 400016） [Abstract] Objective To investigate the preparation of ultrasound microbubbles（MBs）can load simultaneously two anticancer drugs and study their 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 Doxorubicin(DOX) were connected with MBs by biotin–avidin linker system, Characterization of MBs were analyzed by particle size analyzer and fluorescent microscope,UV-visible spectrometer and Multi-function microplate reader were identified the capability of MBs loading PTX and DOX；ultrasound irradiation with different MI were triggered cavitation，the efficiency of releas drug were evaluated through the proportion of the amount of free drug. Results Observed red fluorescent around of MBs that the mean size was(1.45±0.27)μm; Given that 3mg of phospholipid，the maximum of PTX encapsulation efficiency was (54.64 ± 2.98)% and each 1×108 microbubbles contain about (4.5±0.53)μg DOX;when MI=1.0 was used to trigger loaded drug MBs ,the efficiency of PTX and DOX releasing were 80% and 15%,respectively, and 90% microbubbles were broken. Conclusion Ultrsound can promote rel