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The covalent functionalization of graphene oxide (GO) with hyaluronic acid (HA) was successfully accomplished by a facile amidation process.The HA-GO nanosheets with a good aqueous solubility and biocompatibility were characterized FT-IR and UV/Vis spectroscopy.Furthermore,controlled loading of mitoxantrone (MIT) onto the HA-GO via π-π stacking interaction was investigated.The results revealed that drug-loaded nanosheets with high loading efficiency of 50 wt%,exhibited pH-sensitive responses to tumor pH.In order to investigate the dynamic behaviors and targeting ability of HA-GO nanosheets on tumor-bearing mice,near-infrared fluorescent (NIFR) dye Cyanine 7 (Cy7) was encapsulated into the nanosheets for in vivo optical imaging.It demonstrated that HA-GO nanosheets could enhance the targeting and residence time in tumor site.Therefore,the MIT/HA-GO nanosheets may potentially be useful to be further development of synergistic cancer therapy.