© 2022 Elsevier B.V.Nanotechnology has emerged as a promising approach to overcome the obstacles against successful cancer chemotherapy. Herein, biocompatible carbon nanosheets grafted with multi-cyclodextrin were fabricated for doxorubicin delivery to breast cancer cells. Structural characteristics of the nanocarrier were evaluated by FTIR, XRD, MAP, EDS, SEM, TEM, and VSM. Drug-loading and -encapsulation efficiencies were calculated to optimize the formulation. The biocompatibility of synthesized drug-carrier was determined using hemolysis assay and the MTT assay was performed to assess the viability of MCF-7 cells after treatment with various formulations. In-vitro drug release revealed the pH-triggered drug release capability of the drug carrier which can improve the cytotoxic potency of the doxorubicin in the tumor microenvironment. Hemolysis assay indicated the blood biocompatible feature of drug carrier which is further confirmed by cytotoxicity study, while, doxorubicin-loaded drug carrier significantly enhanced the cytotoxic effect of doxorubicin. Fluorescence microscopy observations of the nucleus after DAPI staining indicated the apoptotic-inducing effect of the drug-loaded carrier in comparison to free drug. This can be due to the higher internalization rate of drug-loaded carriers observed in fluorescence microscopy images. These results suggest that the fabricated drug carrier can be considered as a possible tool for the delivery of doxorubicin to breast cancer cells.