Humanized anti-VEGFR-2 ScFv-As2O3-stealth nanoparticles, an antibody conjugate with potent and selective anti-hepatocellular carcinoma activity

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.