Xiangbao Yin, Linquan Wu, Mingwen Huang, Fan Zhou, Kai Wang, Xin Yu, Kaiyang Wang, Huaqun Fu
Department of hepatobiliary surgery, 2(nd) affiliated hospital of Nanchang University, n(o) 1 Minde Road, Nanchang, Jiangxi Province 330006, China.
Department of hepatobiliary surgery, 2(nd) affiliated hospital of Nanchang University, n(o) 1 Minde Road, Nanchang, Jiangxi Province 330006, China.
Biomed Pharmacother. 2014 Jun;68(5):597-602. doi: 10.1016/j.biopha.2014.04.006. Epub 2014 Apr 27.
Low sensitivity of tumor tissue, targeting and sustained release of the drug are bottlenecks of the effect of chemotherapy on hepatocellular carcinoma. In this study, we used the ribosome display technology to screen human anti-VEGFR 2-single-chain antibody (ScFv) that could target directly to VEGFR2, and nanotechnology to prepare As2O3-nanoparticles. Then we built anti-VEGFR-2ScFv-As2O3-stealth nanoparticles using molecular coupling technology, which significantly increased anti-tumor effect while reducing toxicity. The in vivo tissue targeting distribution and anti-tumor effects of the anti-VEGFR-2 ScFv-As2O3-stealth nanoparticles were investigated. Our results showed that anti-VEGFR-2 ScFv-As2O3-stealth nanoparticles could inhibit the development of liver cancer xenograft as a targeting agent and also significantly inhibit angiogenesis.
肿瘤组织的低敏感性、药物的靶向性和缓释性是化疗对肝细胞癌疗效的瓶颈。在本研究中，我们利用核糖体展示技术筛选可直接靶向VEGFR2的人抗VEGFR 2单链抗体（ScFv），并利用纳米技术制备三氧化二砷纳米颗粒。然后我们使用分子偶联技术构建抗VEGFR-2ScFv-As2O3隐形纳米颗粒，其在降低毒性的同时显著提高了抗肿瘤效果。研究了抗VEGFR-2 ScFv-As2O3隐形纳米颗粒的体内组织靶向分布和抗肿瘤作用。我们的结果表明，抗VEGFR-2 ScFv-As2O3隐形纳米颗粒作为靶向剂可抑制肝癌异种移植瘤的生长，还能显著抑制血管生成。
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