High-efficiency anti-tumor nano-drugs refer to anti-cancer drug carriers with special functions and excellent performance prepared by nanotechnology. They can realize accurate diagnosis and treatment of tumors, improve the bioavailability and therapeutic effect of drugs, and reduce the toxic, side effects and resistance of drugs. The design of efficient antitumor nanomedicine needs to consider many factors, including the material, morphology, size, surface modification, drug loading, release mechanism of nanocarrier, as well as the circulation, distribution, targeting, penetration, endocytosis, and escape of nanomedicine in the body.