▎ 摘　　要

pH-responsive chitosan-coated graphene oxide-mesoporous silica nanoparticles (GMSN-Cs) was synthesized as a core-shell nanosheets to be used as DOX delivery system. First of all, an inorganic nanohybrid (GMSN) was prepared and subsequently, chitosan was attached to the mesoporous silica part through firm covalent bonds to form a reliable vector for DOX delivery. The chemico-physical properties of the nanosheets were specified, and DOX-loading efficiency and drug releasing was characterized in different pHs. At lower pH, the cumulative release of DOX-loaded GMSN-Cs was more than physiological pH. The in vitro hemolysis and in vivo biochemical analysis results demonstrate negligible toxicity of GMSN-Cs in mice at a high dosage of nanosheets and a disposal time (up to 10 days). DOX can be loaded efficiently on GMSN-Cs, and the resulting DOX-GMSN-Cs represents meaningful cytotoxicity in different pHs and concentrations for MCF-7 cells. The results and observations confirmed that the drug release of DOX-loaded GMSN-Cs can be controlled by physiological stimulant to reduce the side effects.