iRGD靶向载药脂质体-微泡复合物的制备及其靶向性研究

发布时间：2018-01-05 15:28

本文关键词：iRGD靶向载药脂质体-微泡复合物的制备及其靶向性研究　出处：《中国医院药学杂志》2016年08期 　论文类型：期刊论文

【摘要】：目的:制备iRGD靶向载药脂质体-微泡复合物,研究其靶向性。方法:采用薄膜-超声分散法制备生物素化的iRGD靶向载药脂质体和生物素化的超声微泡。利用生物素-亲和素系统(Biotin-avidin-system,BAS)连接脂质体与微泡,构建并表征iRGD靶向载药脂质体-微泡复合物。细胞黏附实验验证复合物的体外靶向结合性能;构建小鼠乳腺癌移植瘤模型,通过靶组织的药物荧光强度验证复合物的体内靶向性。结果:iRGD靶向载药脂质体的粒径为(165.07±4.01)nm,电位为(-12.92±0.26)mv,复合物的载药量为每108个复合物载紫杉醇(46.22±1.95)μg;黏附实验表明靶向组复合物与血管内皮细胞结合数量明显多于非靶向组复合物(7.8±1.1,0.2±0.45,P0.01);荷瘤小鼠活体成像实验显示靶向组复合物的肿瘤组织荧光明显强于非靶向组复合物。结论:iRGD靶向载药脂质体-微泡复合物,作为一种靶向给药系统,可以实现超声分子成像与超声给药的有机结合,显著提高药物靶向递送的效率。
[Abstract]:Objective: to prepare iRGD targeting liposome-microbubble complexes. Methods: biotinylated iRGD targeting liposomes and biotinylated ultrasound microbubbles were prepared by thin-film ultrasonic dispersion method. Biotin-avidin-system. The liposome-microbubble complexes of iRGD targeting drugs were constructed and characterized. The cell adhesion experiments demonstrated the in vitro targeting binding properties of the complexes. Mouse breast cancer transplanted tumor model was established. The drug fluorescence intensity of the target tissue was used to verify the in vivo targeting of the complex. Results the particle size of the liposome targeting the drug was 165.07 卤4.01 nm. The potential was -12.92 卤0.26mv, and the drug loading capacity of the complex was 46.22 卤1.95 渭 g per 108 complexes. The adhesion test showed that the number of binding between the target group and vascular endothelial cells was significantly higher than that in the non-target group (7.8 卤1.1 卤0.2 卤0.45p 0.01g / L). In vivo imaging of tumor-bearing mice showed that the fluorescence of tumor tissue of the target group complex was significantly higher than that of the non-target group complex. Conclusion: iRGD targeted liposome-microbubble complex as a targeting drug delivery system. The combination of ultrasonic molecular imaging and ultrasonic administration can be realized, and the efficiency of targeted delivery of drugs can be improved significantly.
【作者单位】：佳木斯大学药学院;中国科学院深圳先进技术研究院;齐齐哈尔医学院药学院;
【基金】：国家自然科学基金项目(编号:81371563)
【分类号】：R943
【正文快照】： 乳腺癌是女性常见的恶性肿瘤之一,且我国女性乳腺癌的死亡率呈持续上升趋势[1]。紫杉醇是来源于红豆杉的一种细胞毒性物质,被广泛用于乳腺癌和卵巢癌的治疗[2]。然而普通抗肿瘤化疗药物无法实现在肿瘤部位靶向聚集并渗透到肿瘤的内部,大大限制了药物的疗效[3]。超声微泡爆破介

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