Abstract: Functionalized graphene oxide is prepared based on graphene. It has attracted great interest from all over the world due to its good solubility, biocompatibility, high loading rate, and easy modification. This paper summarizes the surface modification of graphene oxide, and its applications on anti-tumor, antibacteria, anti-hypertension, gene therapy and biosafety as a drug carrier, providing new methods and ideas in the biomedical field.