Abstract: OBJECTIVE To introduce the latest researches about active targeting liposomes. METHODS Review the strategies of adsorbing ligands onto the vector surface, the selection of targeted ligands and the application of active targeting liposomes through searching and summarizing relevant literatures. RESULTS There were three strategies of adsorbing ligands onto the vector surface: addition of ligands as components during the preparation liposomes, direct coupling method, and post insertion method. Active targeting of liposomes could deliver the cargo to target cells, tissues and even the intracellular localization, which could improve the drug bioavailability and produced no increase in toxicity towards normal tissue or cells. The drug-delivery system had become one of the most widely study of targeting drug-deliver systems in recent years. CONCLUSION The active targeting liposomes is a very promising drug delivery system.