Dual-labeled galactosylated chitosan-graft-poly(ethylene glycol) (PEG) (GCP)/DNA complexes were prepared and their hepatocyte-specific delivery and cellular distribution were investigated by confocal laser scanning microscopy (CLSM). The complexes were transfected into hepatocyte through specific interaction of galactose moiety of the GCP and asialoglycoprotein receptors (ASGPR) of the hepatocytes. The GCP/DNA complexes taken up by the hepatocytes were rapidly released into the cytoplasm, but nuclear trafficking of the released complexes was slow and rate-limiting process. The more efficient transfection of the complex occurred in the human-derived HepG2 cells than in primary hepatocytes.