Nowadays, the concept of drug transmission is an important topic in the field of drug delivery research. Drug delivery is the method or process of administering a pharmaceutical compound to achieve a therapeutic effect in humans or animals. In this study, we report the development of a novel platform for the loading and release of doxorubicin (DOX). It is based on porous reduced graphene oxide (prGO) nanosheets and chitosan (CS) biocompatible polymer, where prGO can be dispersed in chitosan through amide linkages. The loading and release of DOX on the CS-prGO nanocomposite were investigated by voltammetry, FE-SEM, and FTIR and UV-Vis spectroscopy methods. We showed that chitosan-modified prGO (CS-prGO) was an extremely efficient matrix. An efficient loading of DOX (86% at pH 7.00, time 3 h and initial concentration of 0.5 mg mL-1) was observed on CS-prGO as compared to the case of prGO due to the presence of the–OH and–NH2 groups of chitosan. At the normal physiological pH of 7.00, approximately 10% of DOX could be released from CS-prGO in a time span of 1 h; however, when exposed to pH 4.00, 25% of DOX was released in 1 h. After 20 h, 18% and 62% of DOX was released at pH 7.00 and 4.00, respectively. This illustrates the major benefits of the developed approach for biomedical applications.