Abstract: Synthetic lipoproteins are efficient nanovectors for targeting delivery of biological drugs, chemical drugs and imaging contrast agents and so on. They have ultra-small particle size, excellent biocompatibility, favorable circulation half-life and specific lipoprotein-receptors-binding capacity of lipoprotein receptors. Compared with traditional natural lipoproteins, synthetic lipoproteins possess both native biochemical properties and functions, and superior drug delivery potentials. This paper introduces the development of lipoproteins as drug nanovectors and reviews preparation methods of synthetic lipoproteins, in vitro and in vivo applications and the approaches employed to expand the limited applications of lipoproteins as drug nanovectors. Further development of synthetic lipoproteins is also proposed.