Disclosed is a composite. The composite comprises a nanocarrier and targeting molecules coupled to a surface of the nanocarrier. The particle size of the nanocarrier is smaller than 200 mn, and the polydispersity index (PDI) is smaller than 0.5. Also disclosed are an antitumor medicament comprising the composite and antitumor drug carried in the nanocarrier of composite, a preparation method therefor, and uses thereof. The composite can convey the antitumor drug into a tumor cell, and has a strong killing effect to the tumor cell.
