碳酸酐酶Ⅸ抗体修饰去甲斑蝥素纳米胶束的肺靶向性研究

发布时间：2018-04-22 19:46

本文选题：去甲斑蝥素 + 碳酸酐酶Ⅸ　；参考：《中药药理与临床》2017年01期

【摘要】：目的:制备碳酸酐酶Ⅸ抗体修饰的去甲斑蝥素纳米胶束(anti-CA IX NCTD nano-micelle),探讨并比较其与普通去甲斑蝥素纳米胶束(NCTD nano-micelle)的抗肿瘤作用。方法:将碳酸酐酶Ⅸ抗体孵化修饰去甲斑蝥素纳米胶束,考察其载药率、包封率、粒径等指标;通过MTT法考察去甲斑蝥素及载药胶束对A549的细胞生存率为细胞摄取实验剂量设置提供依据;取荷瘤裸鼠分别尾静脉注射去甲斑蝥素和载药胶束,并观察裸鼠的饮食,精神状态,每周用游标卡尺测量肿瘤的大小,绘制肿瘤生长曲线。结果:制备的碳酸酐酶Ⅸ抗体修饰的去甲斑蝥素纳米胶束呈圆球状,载药量为(1.26±0.03)%,包封率为(80.93±1.01)%,粒径和Zeta电位分别为146.5±48.9nm,-(14.79±0.67)mv;去甲斑蝥素及载药胶束对肿瘤细胞的抑制作用呈剂量和时间依赖性,载药胶束对肿瘤细胞的抑制作用明显优于游离药物,且anti-CA IX NCTD nano-micelle对A549的抑制率优于NCTD nano-micelle。结论:去甲斑蝥素纳米胶束经碳酸酐酶Ⅸ抗体修饰后能达到主动靶向的效果,同时能与去甲斑蝥素协同抑瘤,起到一举多得的目的。
[Abstract]:Aim: to prepare anti-CA IX NCTD nano-micelle modified by carbonic anhydrase IX antibody and compare its antitumor effect with that of norcantharidin nano-micelle (NCTD nano-micelle). Methods: the nanoparticles of norcantharidin were incubated with carbonic anhydrase IX antibody, and the drug loading rate, encapsulation efficiency and particle size were investigated. The survival rate of A549 cells was determined by MTT method, and the dose-setting of cell uptake was determined by using norcantharidin and drug carrier micelles, and the nocantharidin and drug carrier micelles were injected into the tail vein of nude mice, and the diet and mental state of the nude mice were observed. The tumor size was measured weekly with Vernier calipers and the tumor growth curve was drawn. Results: the norcantharidin nanoparticles modified by carbonic anhydrase IX antibody were spherical. The drug loading amount was 1.26 卤0.03g, the encapsulation efficiency was 80.93 卤1.01g, the particle size and Zeta potential were 146.5 卤48.9nmg-0.79 卤0.67mv.The inhibitory effect of norcantharidin and drug carrier micelles on tumor cells was dose-and time-dependent, and the inhibitory effect of drug-loaded micelles on tumor cells was obviously superior to that of free drugs. The inhibition rate of A549 by anti-CA IX NCTD nano-micelle was better than that of nano- micelle. Conclusion: after modified with carbonic anhydrase IX antibody, norcantharidin nanoparticles can achieve active targeting effect, and can cooperate with norcantharidin in inhibiting tumor.
【作者单位】：苏州卫生职业技术学院;苏州大学医学部药学院;香港浸会大学中医药学院;苏州市吴中区人民医院肿瘤科;
【基金】：江苏省卫生厅资助项目:抗肿瘤药物去甲斑蝥素靶向制剂的制备研究(JZ201402) 2016年江苏省高校"青蓝工程"优秀骨干教师培养对象资助项目
【分类号】：R943

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