In summary, 131I-antiAFPMcAb-GCV-BSA-NPs have been prepared successfully for the first time in the present study. In vitro and in vivo experiments confirmed the highly selective targeting of 131I-antiAFPMcAb-GCV-BSA-NPs to AFP-positive hepatocellular carcinoma tissue or cells. This evidence concerns the gene AFP and hepatocellular carcinoma.