This study examined the optical characteristics of bicalutamide-loaded magnetic/ethylene glycol composite nanoparticles (BMP), as well as their anti-cancer activity against cancer cells. The gamma-Fe2O3 magnetic nanoparticles (MNPs), approximately 20 nm in diameter, were prepared via a chemical co-precipitation method and coated with two surfactants to yield a water-based product. The characteristics of the particles were determined via X-ray diffraction (XRD), field emission scanning electron microscopy, and Raman spectrophotometry. The Raman spectra of the BMP showed peaks at 222, 283, 395, 520, 669 and 1316 cm(-1), with broadened band in comparison to the Raman spectra of the magnetic nanoparticles. The BMP absorbance evidenced a rapid increase, with a broad peak at 409 nm, thus reflecting a good loading of the bicalutamide onto the magnetic nanoparticles. The results of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay showed that the MNPs were non-toxic against human brain cancer cells (SH-SY5Y), human cervical cancer cells (Hela), human liver cancer cells (HepG2), breast cancer cells (MCF-7), colon cancer cells (CaCO2) and human prostate cancers (Du 145, PC3) tested herein. In particular, BMPs were cytotoxic at 56% against DU145 cells, at 74.37% in SH-SY5Y cells, and at 58% in Hela cells. Our results demonstrated the biological applicability of BMP nanoparticles as anticancer agents and as agents for enhanced drug delivery against human prostate cancer cells. Our results indicated that the MNPs were biostable and that the BMP functioned effectively as drug delivery vehicles.