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Polymers bearing pendant galactosyl group are attractive for targeted intracellular antitumor drug delivery to hepatoma cells (e.g. HepG2 and SMMC7721 cells) with asialoglycoprotein receptor (ASGP-R). Herein, a series of galactopeptides was synthesized through ring-opening polymerization of L-glutamate N-carboxyanhydride, deprotection of benzyl group and subsequent Huisgens cycloaddition “click” reaction with azide-modified galactosyl group. The copolypeptides were revealed to have excellent hemocompatibilities, and cell and tissue compatibilities, which rendered their potential for drug delivery applications. The hepatoma-targeted micellar nanoparticle (i.e. nanomedicine) was fabricated by cooperative self-assembly of galactopeptide and doxorubicin (DOX) induced by two-stage physical interactions. In vitro DOX release from nanomedicine was accelerated in the intracellular acidic condition. Through the recognition between galactose ligand and ASGP-R of HepG2 cells, the endocytosis of galactosylated nanomedicine was significantly promoted, which was demonstrated by confocal laser scanning microscopy and flow cytometry. Remarkably, the galactose-decorated nanomedicine retained much higher antitumor activity toward HepG2 cells in contrast to the nanomedicine without galactosyl group in vitro and in vivo. The above superiorities indicated that the galactosylated nanomedicine possessed great promising for hepatoma-targeted chemotherapy.