Hepatic diseases are turning into one of the few diseases that cannot be effectively cured due to some reasons although various receptors existed in the liver. Currently, several passive targeting delivery systems have been used in the drug/gene delivery for the treatment of hepatic diseases. For example, Zinostatin stimalamer (trade name of Smancs(®)), a drug-polymer conjugate, was launched in Japan in 1994, which treats hepatocellular carcinoma. More improtantly, different measures would be taken in accord to the specified cell that was lesioned or dysfunctioned via interaction between homing ligands and target receptors so as to improve accumulation of drugs in the target cell and to reduce nonspecific toxicity towards other cells or organs. Therefore, it is urgent to design novel delivery systems that physically or chemically grafted homing devices in order to improve the targeting properties of drugs in specific cell sites. From that perspective, the present article highlights recent development of active hepatic targeting drug/gene delivery systems for the treatment of hepatic diseases that were mediated by some kinds of receptors including asialoglycoprotein receptors (ASGP-R), glycyrrhetinic acid receptor (GA-R), glycyrrhizin receptor (GL-R), hyaluronan receptor (HA-R) and so on.