Innovative drug delivery platforms for selective, regulated, and sustained release of anticancer drugs are crucial in cancer treatment. This study presents nanoparticles developed from chitosan (CS), graphene oxide (GO), and magnetite (FeO), and their nanocomposites to enhance the loading and release efficiency of camptothecin (CPT). Nanostructures were characterized using imaging microscopy, FT-IR, and X-ray diffraction, with an average crystallite size of 5.5 nm. Camptothecin binding proportions were 70 % for CS, 81 % for CS@FeO, 58 % for CS@GO, and 74 % for CS@GO/FeO. At pH 5.0, CPT release ratios were 87 %, 80 %, 88 %, and 90 %, respectively, and at pH 7.4, 84 %, 72 %, 89 %, and 87 %. Cytotoxicity was assessed using the MTT assay against HepG2 and SMMC-7721 cancer cells. CPT-CS@GO/FeO exhibited the highest survival at 5 μM and 12.5 μM concentrations, indicating it as the most effective nanocarrier for camptothecin delivery. The study demonstrates CS@GO/FeO's potential as a superior drug delivery system.