The objectives of this study were to develop a gentle and facile method to fabricate conjugated linolenic acid (CLnA)-modified, bovine serum albumin (BSA)-linked, magnetic gamma-Fe2O3 nano-composites and to give a preliminary assessment of its in vitro antineoplastic activity, in vivo pharmacokinetics and bio-distribution. Fourier transform infrared spectra and transmission electron microscopy indicated that albumin was the key to controlling the final product size and supplying sites for the CLnA linkage. The magnetic nano-composites had diameters of 45.7 +/- 14.8 nm and a negatively charged surface. The nano-composites maintained stability against oxidation and aggregation in vitro for 12 h. Additionally, both the metabolic and morphological tests revealed that the magnetic nano-composites could inhibit the metabolism and proliferation of human hepatocarcinoma cells and mouse embryonic fibroblast cell line in a dose-dependent manner, with 303 ppm and 254 ppm of the half maximal inhibitory concentration (IC50), respectively. However, rat pheochromocytoma cells were not sensitive to nano-composites. BALB/c mice that were intravenously injected with doses of 250 mu mol Fe/kg could rapidly eliminate the magnetic nano-composites from the serum, with a half-life of 0.62 h. The elimination rate in the other tissues was in the order of kidney < heart < liver, spleen and lung < whole blood. With these findings, the present study substantiated the potential of CLnA-modified BSA-linked magnetic gamma-Fe2O3 nano-composites as an antineoplastic drug. (C) 2014 Elsevier B.V. All rights reserved.