In this study, the anti-tumor activity of hederagenin-loaded magnetic nanoparticles (HMP) was examined in cancer cells. Composite nanoparticles with an average size of 32.5 nm were prepared using a chemical co-precipitation technique. The characteristics of the particles were determined via X-ray diffraction, field emission scanning electron microscopy, attenuated total reflectance fourier transform-infrared spectroscopy, and energy-dispersive X-ray spectroscopy. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay showed that the magnetic nanoparticles were non-toxic against cancer. In particular, HMPs were cytotoxic at 73.12 % breast cancer (MCF-7), at 70.2 % against prostate cancer (DU145 cells), at 72.15 % against neuroblastoma cancer cells (U87), at 579.15 % in human brain cancer cells (SH-SY5Y), and at 74.5 % in human cervical cancer cells (HeLa) at 250 mg/mL. Our results demonstrated the biological applicability of HMPs as anticancer agents and as agents for enhanced drug delivery against human prostate cancer cells. Our results indicate that the magnetic nanoparticles were biostable and that HMPs functioned effectively as drug delivery vehicles.