This research aims to design and synthesize a drug contained nanocomposite papered with a new combination of chitosan (CS)-coated magnetic-gold core-shell (Fe3O4@Au) as curcumin (CU) delivery to treat breast cancer (MDA-MB-231) and normal (MCF10A) cell lines. The CU drug was encapsulated in this nanosystem. Folate (Fol) functionalization of this nanosystem for targeting therapy purposes led to the construction of the final Fe3O4@Au-CS-CU-Fol nanoformulation. The SPION@Au was achieved using Pulsed Laser Ablation in Liquid (PLAL) procedure by the 530 nm wavelength with various laser fluence (1.8, 2.3, and 2.6) J/cm2. The polymeric coating, drug encapsulation, and Fol functionalization processes were performed due to reverse microemulsion methods. This nanosystem was characterized by a dynamic light scattering (DLS) Atomic Force Microscope (AFM), Field Emission Scanning Electron Microscopy (FESEM), High-Resolution Transmission Electron Microscopy (HRTEM), UV-Visible spectrophotometer, and vibrating sample magnetometry (VSM). A new type of CU-loaded nanocarrier was synthesized, and its anti-tumor properties were evaluated against breast cancer cell lines in both in vitro and in vivo conditions. The obtained mean size of Fe3O4@Au nanoparticles (NPs) was 52.37, 60.24, and 72.45 nm at 1.8, 2.3, and 2.6 J/cm2, respectively. The MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay of drug-loaded NPs on the MDA-MB-231 cell line proved that the CU cytotoxicity effect could enhance when encapsulated in Fe3O4@Au-CS-Fol nanocarrier compared with void CU. On the other hand, the flow cytometry charts presented that this nanoformulation can enhance the remedial properties of CU due to apoptosis stimulation in the MDA-MB-231 cell line. The real-time polymerase chain reaction (PCR) analysis confirmed the activation of apoptosis in the cells treated with the Fe3O4@Au-CS-CU-Fol. The in vivo evaluation of the Fe3O4@Au-CS-CU-Fol nanosystem proved that the tumor volume reduces in a certain time. Close inspection of results confirmed that Fe3O4@Au-CS-CU-Fol exerts a significant chemo-preventive effect on breast cancer through cell viability index, apoptosis stimulation, and anti-tumor activity.