| 骆杰,王志刚,张群霞,钟世根,张辉.载10-羟基喜树碱靶向脂质微泡的制备及体外寻靶能力实验研究[J].中国医学影像技术,2010,26(3):418~420 |
| 载10-羟基喜树碱靶向脂质微泡的制备及体外寻靶能力实验研究 |
| Experimental study on preparation and targeting ability in vitro of HCC-targeted lipid microbubble containing 10-HCPT |
| 投稿时间：2009-09-28 修订日期：2009-11-18 |
| DOI： |
| 中文关键词: 10-羟基喜树碱 抗体,单克隆 微泡 |
| 英文关键词:10-hydroxycamptothecin Antibodies, monoclonal Microbubbles |
| 基金项目:国家自然科学基金面上项目(30770566、30970752)。 |
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| 中文摘要: |
| 目的 制备携人肝癌单抗Hab18载10-羟基喜树碱的脂质微泡,并观察其体外寻靶能力。方法 制备生物素化抗人肝癌Hab18单克隆抗体,检测其生物素化程度;用机械振荡法制备载药脂质微泡,以生物素-亲和素桥连方式构建携人肝癌单抗Hab18载10-羟基喜树碱的脂质超声微泡,检测其一般特性、包封率和载药量,以免疫荧光法检测微泡与抗体的连接情况,在光镜下观察靶向载药微泡的寻靶能力,并与载药非靶向微泡进行比较。结果 每个单抗分子平均可与13个生 物素分子结合。载药靶向脂质超声微泡分布均匀,平均粒径为1.52 μm,包封率为76.32％,载药量为21.81％。免疫荧光法显示微泡表面可见明亮的红色环状荧光,体外寻靶实验显示该载药靶向微泡可与人肝癌7721细胞牢固结合。结论 携人肝癌单抗Hab18载10-羟基喜树碱的脂质超声载药靶向微泡可成功制备,其包封率和载药量较高,具有较强的体外寻靶能力。 |
| 英文摘要: |
| Objective To prepare HCC-targeted lipid ultrasound microbubble containing 10-hydroxycamptothecin (10-HCPT), and to assess its targeting function in vitro. Methods After the biotinylated monoclonal antibody Hab18 was prepared, the biotinylated degree was determined. Microbubbles containing 10-HCPT were prepared by mechanical vibration. Then the biotinylated antibody was attached to the surface of the microbubbles by avidin-biotin interaction. The physical property, entrapment efficiency and the drug-loading amounts of 10-HCPT lipid microbubbles were determined. The combination of biotinylated Hab18 with microbubbles containing 10-HCPT was proved by immunofluorescent assay, and the targeting function of the targeted microbubbles containing 10-HCPT was observed with light microscope, served non-targeted microbubbles as control group. Results About 13 biotin molecules were coupled to each antibody in average. The disposition of the prepared microbubbles was steady and the mean diameter was 1.52 μm. The drug entrapment efficiency was 76.32% and the drug-loading amounts was 21.81%. Red fluorescence was observed at the edge of the microbubbles in immunofluorescent assay, and the conjugation of the targeted microbubbles containing 10-HCPT with 7721 cells was tight while control group was negative. Conclusion HCC-targeted lipid ultrasound microbubbles containing 10-HPTC can be prepared successfully, with higher entrapment efficiency and drug-loading amounts and strong targeting function in vitro. |
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