▎ 摘　　要

A novel phosphorylcholine oligomer-grafted and folate moiety-labeled graphene oxide (GO-PCn-FA) was designed, prepared, and characterized by Fourier transform infrared spectra, nuclear magnetic resonance, Raman spectra, X-ray diffraction, X-ray photoelectron spectroscopy, scanning transmission electron microscopy, transmission electron microscopy, and atomic force microscopy. GO-PCn-FA proved to be an excellent water-soluble and pH-responsive drug carrier for the targeted delivery of doxorubicin (DOX) with a drug loading content of 21%. An in vitro cytotoxicity assay and flow cytometry analysis revealed the superior biocompatibility of GO-PCn-FA compared to normal cells, while DOX-loaded GO-PCn-FA exerted efficient eradication of tumor cells, especially of those with folate receptor expression. An in vivo test showed that GO-PCn-FA was deposited mainly in the pulmonary parenchyma after intravenous administration, and no obvious adverse effect was observed. In summary, phosphorylcholine oligomer-grafted graphene oxide was developed for targeted drug delivery with optimal biocompatibility.