▎ 摘　　要

Introduction: As a shining star in material science, graphene oxide (GO) and its derivatives possess potential applications in a variety of areas. Among them, the application of GO to drug delivery has attracted ever-increasing interest in the past few years. Areas covered: In this article, the authors summarize the latest progress of utilizing GO in the field of drug delivery. In particular, the functionalization of GO, cytotoxicity of GO and its derivatives, in vitro and in vivo drug delivery and the comparison with carbon nanotube-based delivery systems are discussed. Future perspectives and possible challenges in this emerging field are briefly described. Expert opinion: GO and its derivatives are highly attractive for the application to drug delivery due to their exceptional physiochemical properties and unique planar structure in spite of some existing challenges, such as the reproducibly smart functionalization of GO and the investigation of its long-term toxicology.