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以碳酸酐酶Ⅸ抗体(anti-CAⅨ)为靶头,采用透析法制备去甲斑蝥素纳米胶束并考察其载药率、包封率、粒径等指标及抗肿瘤靶向性。结果表明,anti-CAⅨ修饰的去甲斑蝥素纳米胶束呈圆球状,载药量、包封率、粒径和ζ电位分别为(5.26±0.03)%、(80.93±1.01)%、(146.5±48.9)nm和(-14.79±0.67)mV。去甲斑蝥素及其anti-CAⅨ修饰的胶束对A549肿瘤细胞在体外的抑制作用呈剂量和时间依赖性,载药胶束的抑制作用明显优于游离药物。荷A549肿瘤的裸鼠体内试验也表明,anti-CAⅨ修饰的去甲斑蝥素纳米胶束能显示出主动靶向效果,高剂量组(1 mg/kg)的抑瘤率达到75.65%。
Norcantharidin nanomicelles were prepared by dialysis using anti-CA IX as a target. The drug-loading rate, entrapment efficiency, particle size and other anti-tumor targets were investigated. The results showed that the anti-CAⅨ modified nornicasanil nanospheres were spherical, the drug loading, entrapment efficiency, particle size and zeta potential were (5.26 ± 0.03)%, (80.93 ± 1.01)%, ± 48.9) nm and (-14.79 ± 0.67) mV. The inhibitory effect of norcantharidin and its anti-CAⅨ modified micelles on A549 tumor cells in vitro was dose-and time-dependent, and the drug-loaded micelles showed significantly better inhibitory effect than the free drug. In vivo experiments of A549 tumor bearing nude mice also showed that the anti-CAⅨ modified norcantharidin nanomicelles showed active targeting effect, and the inhibition rate of high dose group (1 mg / kg) reached 75.65%.