mGO was prepared by chemical co-precipitation of Fe3O4 MNP on GO nano-platelets. mGO was further modified by chitosan and mPEG-NHS to synthesize mGOC-PEG. mGOC-PEG showed higher drug loading of doxorubicin (DOX) than irinotecan. mGOC-PEG showed pH-responsive controlled release of chemotherapy drugs. Magnetic targeting enhanced cytotoxicity of mGOC-PEG/DOX toward U87 cancer cells.