This research presents the synthesis of graphitic carbon nitride (GCN) followed by its functionalization with diglycolamic acid (GCD) to enhance its role as a carrier for cisplatin in cancer treatment. Compared to GCN, which had drug content and cisplatin loading efficiencies of 26% and 13% respectively, the GCD achieved higher values of 34% and 68%. The success of the functionalization and drug conjugation process was confirmed through comprehensive characterization using techniques such as UV-Visible spectroscopy, FTIR, DLS, SEM, EDAX, XPS, ICP-MS, and solid state ¹³ C NMR. In vitro drug release studies revealed that the cisplatin conjugated GCD (GCDC) compound exhibited pH-responsive behavior, maintaining prolonged retention at physiological pH and increased release of cisplatin in acidic tumor-like environments. Hemolysis and biocompatibility studies indicated that GCDC has improved hemocompatibility and reduced cytotoxicity toward fibroblast cells, while maintaining strong anticancer activity against MCF-7 breast cancer cells. AO/EB staining and cytotoxicity assay demonstrated that GCDC more effective in inducing controlled apoptosis than the cisplatin-bound pristine GCN (GCNC) system. These results highlight the promise of diglycolamic acid-functionalized graphitic carbon nitride as a effective and biocompatible carrier for enhanced and controlled cisplatin delivery in chemotherapy.