The results of an in vitro cell uptake study and an in vivo biodistribution study revealed a promising new vehicle for targeting liver tumor chemotherapy in which doxorubicin-loaded GA-HSA nanoparticles increased cytotoxic activity in HepG2 cells in vitro and exhibited a much higher level of tumor accumulation in hepatoma (H22 cell)-bearing mice. This evidence concerns the gene ALB and hepatocellular carcinoma.