▎ 摘　　要

Graphene-based nanomaterials have exhibited wide applications in nanotechnology, materials science, analytical science, and biomedical engineering due to their unique physical and chemical properties. In particular, graphene has been an excellent nanocarrier for drug delivery application because of its two-dimensional structure, large surface area, high stability, good biocompatibility, and easy surface modification. In this review, we present the recent advances in the synthesis and drug delivery application of graphene-based nanomaterials. The modification of graphene and the conjugation of graphene with other materials, such as small molecules, nanoparticles, polymers, and biomacromolecules as functional nanohybrids are introduced. In addition, the controlled drug delivery with the fabricated graphene-based nanomaterials are demonstrated in detail. It is expected that this review will guide the chemical modification of graphene for designing novel functional nanohybrids. It will also promote the potential applications of graphene-based nanomaterials in other biomedical fields, like biosensing and tissue engineering.