Abstract: Currently, targeted drug delivery system is an effective method to treat cancer, and the selection of targeted ligands is the key of targeted drug delivery. Biotin receptors are over-expressed on the surface of most tumor cells, but lowly or under-expressed in normal cells. This article briefly introduces biotin and biotin receptors, and further reviews the research progress of diagnosis and treatment of cancer using biotin modified liposomes, micelles, nanoparticles and other drug delivery systems in order to provide reference for related research and clinical application.