Asialoglycoprotein receptor-targeted liposomes loaded with a norcantharimide derivative for hepatocyte-selective targeting

•Asialoglycoprotein receptor-targeted liposomes loaded with a norcantharimide derivative were successfully prepared with a high EE%.•In comparison with conventional liposomes, GAL-Lipo displays increased specific active targeting of hepatocellular carcinoma.•GAL-Lipo is internalized into Hep G2 cells by caveolin-dependent endocytosis and clathrin-dependent ASGP-R mediated endocytosis.•PEGylated liposomes can effectively increase the AUC and prolong the half-life of N-14NCTDA in vivo.•GAL-Lipo could effectively reduce renal and hepatocellular toxicity.