Here, we report the synthesis, characterization and the impact of magnetite nanoparticles functionalized with cytostatic drugs, epirubicin (Epi) and fludarabine (Flu) (Fe3O4@Epi, Fe3O4@Flu) prepared by chemical co-precipitation method on tumoral cells in vitro. The average diameter of the resulted particles was about 4 nm for both Fe3O4@Epi and for Fe3O4@Flu. These bioactive nanostructured materials proved to significantly enhance the antitumor effect of tested cytostatic drugs in vitro. The most significant result was obtained in the case of Epi, where the tested magnetite nanostructured material enhanced the cytotoxic effect of this drug with more than 50%.