▎ 摘　　要

The sequential functionalization of graphene (Gr) with oleylamine (ODA) and diethanolamine (DEA) was performed to produce amphiphilic Janus-type graphene nanosheets (DEA-f-Gr-f-ODA). The Janus graphene was self assembled in 3D superstructures with hydrophilic external surface and hydrophobic internal space. The DEA-f- Gr-f-ODA nanoparticles were investigated as platforms for the hydrophobic anticancer drug camptothecin (CPT). The colloidal stability, drug loading and drug release properties of the DEA-f-Gr-f-ODA nanoparticles were determined. The viability of A549 cancer cells in the presence of increasing concentrations of free CPT and blank and drug-loaded DEA-f-Gr-f-ODA nanoparticles was assessed with MTT accompanied with PI/Annexin-V apoptosis assessment with flow cytometry. The uptake of DEA-f-Gr-f-ODA nanoparticles by the A549 cells was also evaluated with flow cytometry. The hemocompatibility of DEA-f-Gr-f-ODA nanoparticles was assessed with a hemolysis assay. The Janus graphene nanoparticles could host an exceptionally large amount of CPT, achieving more than double CPT loading compared to graphene-based CPT platforms reported so far, and released it in a slow biphasic fashion. The cytotoxicity and hemolysis assays provided evidence for the biocompatibility of the DEA-f-Gr-f-ODA nanoparticles and the CPT-loaded DEA-f-Gr-f-ODA nanoparticles were more cytotoxic against a human cancer cell line than free CPT, inducing a higher degree of apoptosis to the cancer cells.