Improvements in the diagnosis and treatment of cancer are urgently needed for use in nanotechnology. Nanoparticles (NPs) can reduce the side effects of traditional chemotherapy by sustained release of loaded drugs and increase therapeutic efficiency. NPs can also enhance endothelial permeation retention by size effect and its accumulation in tumor cells through passive targeting. Furthermore, it is critical to treat cancer with a controlled targeted drug which can be specifically delivered into tumor cells and released there, resulting in a targeted therapy to eradicate tumor cells while sparing normal cells. To this end, antibody-mediated targeting therapy has been developed, but imperfections in antibodies (Abs) limit this therapy. Therefore, the combination of NPs and Abs has been highly valued in recent years, because conjugating special Abs on the surface of NPs can increase targeting efficiency, enabling selective delivery of anti-cancer drugs to tumor cells. In this mini-review, we would like to enumerate the strategies for the conjugation of Abs to the surface of the NPs as well as the precise engineering of targeted NPs. The application of targeting antibody fragments in this drug delivery system will also be discussed.