【摘要】：以碳酸酐酶Ⅸ抗體(anti-CAⅨ)為靶頭,采用透析法制備去甲斑蝥素納米膠束并考察其載藥率、包封率、粒徑等指標及抗腫瘤靶向性。結(jié)果表明,anti-CAⅨ修飾的去甲斑蝥素納米膠束呈圓球狀,載藥量、包封率、粒徑和ζ電位分別為(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修飾的膠束對A549腫瘤細胞在體外的抑制作用呈劑量和時間依賴性,載藥膠束的抑制作用明顯優(yōu)于游離藥物。荷A549腫瘤的裸鼠體內(nèi)試驗也表明,anti-CAⅨ修飾的去甲斑蝥素納米膠束能顯示出主動靶向效果,高劑量組(1 mg/kg)的抑瘤率達到75.65%。
[Abstract]:Using carbonic anhydrase IX antibody (anti-CA IX) as target, norcantharidin nano-micelles were prepared by dialysis method and their drug loading rate, encapsulation efficiency, particle size and anti-tumor targeting were investigated. The results showed that the nanoparticles modified by anti-CA IX were spherical, with drug loading, encapsulation efficiency, particle size and 味 potential of (5.26 鹵0.03)%, (80.93 鹵1.01)%, (146.5 鹵48.9) nm and (-14.79 鹵0.67) mV., respectively. The inhibitory effect of norcantharidin and its modified micelle anti-CA IX on A549 tumor cells in vitro was dose-and time-dependent, and the inhibitory effect of drug-loaded micelle was better than that of free drug. In vivo experiments in nude mice bearing A549 tumor also showed that the anti-CA IX modified norcantharidin nanoparticles could show active targeting effect, and the inhibitory rate of high dose group (1 mg/kg) reached 75.65%.
【作者單位】： 蘇州衛(wèi)生職業(yè)技術(shù)學(xué)院藥物制劑教研室;蘇州大學(xué)醫(yī)學(xué)部藥學(xué)院;香港浸會大學(xué)中醫(yī)藥學(xué)院;蘇州市吳中區(qū)人民醫(yī)院腫瘤科;
【基金】：江蘇省衛(wèi)生廳資助項目《抗腫瘤藥物去甲斑蝥素靶向制劑的制備研究》(JZ201402) 2016年度江蘇高�！扒嗨{工程”培養(yǎng)對象資助項目
【分類號】：R943
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本文編號：2285471