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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 lipid microbubbles that can simultaneously carry two kinds of anti-tumor drugs and study their drug loading capacity and in vitro release control. Methods Lipid microbubbles were prepared by mechanical vibration method, paclitaxel was loaded by embedding method and the doxorubicin liposomes were attached by biotin-avidin system. Particle size analyzer and fluorescence microscopy for characterization analysis, UV spectrophotometry and microplate reader were measured paclitaxel and doxorubicin drug loading; Under ultrasound irradiation, to promote the release of paclitaxel and doxorubicin microbubbles, And determine their drug release to determine the drug release efficiency of ultrasound irradiation microbubbles. Results The particle size of drug-loaded microbubbles was (1.45 ± 0.27) μm, and the red fluorescence around the microbubbles was observed under fluorescence microscope. The maximum entrapment efficiency of paclitaxel with 3 mg fixed phospholipid was 54.64 ± 2.98)%, and the amount of doxorubicin was (4.52 ± 0.53) μg per 108 microvesicles. When the mechanical index of ultrasound was 1.0 (MI = 1.0), 90% microbubbles were broken and the release of paclitaxel and doxorubicin Rates were 15% and 80% respectively. Conclusion The drug-loaded microbubbles have good drug release ability under ultrasonic irradiation and can provide an effective double drug carrier for the treatment of tumor in the auxiliary system of ultrasound imaging.