INTRODUCTION: Doxorubicin (DOX) is one of the most common drugs in cancer treatment. However, its partial solubility along with the high incidence of side effects remains a challenge to tackle. To address these issues, we designed a formulation based on graphene oxide (GO) and used it as an anticancer drug delivery system. METHODS: The physical and chemical properties of the formulation were studied using FTIR, SEM, EDX, Mapping, and XRD. Release studies in the condition were used to evaluate the pH sensitivity of drug release from nanocarriers. Other studies, including uptake assay, MTT, and apoptosis assay were carried out on the osteosarcoma cell line. RESULTS: release studies confirmed that the synthesized formulation provides a better payload release profile in acidic conditions, which is usually the case in the tumor site. On the OS cell line, the cytotoxicity of the DOX-loaded nanocarrier (IC50=0.293 μg/mL) and early apoptosis rate (33.80 % ) were higher in comparison to free DOX (IC50=0.472 μg/mL, and early apoptosis rate= 8.31 % ) after 48 hours. CONCLUSION: In summary, our results suggest a DOX-loaded graphene oxide carrier as a potential platform for targeting cancer cells.