AIM & BACKGROUND: Increased efficacy with reduced side effects in cancer treatment is achieved through targeted distribution of anti-cancer medications. Because of their biocompatibility, biodegradability, low toxicity, and target ability under magnetic field, magnetic nanoparticles (MNP) based chitosan nanocomposite have attracted attention among other delivery technologies. METHODOLOGY: MNPs were synthesised using the co-precipitation method. After the successful synthesis of MNPs, it was successfully encapsulated with 5-fluorouracil (5-FU) within chitosan beads, making it ideal for targeted drug delivery to treat breast cancer cells. The properties of MNP-based drug-loaded chitosan nanocomposite were characterised by various characterization techniques like scanning electron microscopy (SEM), high-resolution transmission electron microscopy (HRTEM), Fourier-transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), vibrating sample magnetometry (VSM), atomic force microscopy (AFM). Entrapment efficiency and cytotoxicity studies of MNP-based drug-loaded chitosan nanocomposites by MTT were also conducted. The release study of the drug from MNP-based drug-loaded chitosan nanocomposite under different pH conditions was also investigated. RESULTS: Instrumental analysis showed successful preparation of MNP-based drug-loaded chitosan nanocomposite. The entrapment efficiency of MNP-based drug-loaded chitosan nanocomposite was 85 % to 90 %. MTT study also proved its toxicity against breast cancer cells, and with increased concentration percentage, cell viability decreases. The release study showed that the release of the drug from MNP-based drug-loaded chitosan nanocomposite varied under different pH conditions. CONCLUSION: Hence, MNP-based drug-loaded chitosan nanocomposite has the potential to be utilised as a targeted drug delivery vehicle for the treatment of breast cancer cells.