This paper describes the preparation of magnetic nanoparticles modified with polyethylenimine (PEI)-folic acid (PF) conjugate and their potential biomedical applications. Magnetic nanoparticles modified with (3-(2-aminoethylamino)propyltrimethoxysilane) (AEAPS) were first prepared using a ligand exchange method to provide biocompatibility and hydrophilicity, and. further conjugated with PF to carry gene and enhance specific uptake into cancer cells. We demonstrated the feasibility of the multifunctional magnetic nanoparticles as contrast agents in magnetic resonance imaging (MRI) and as gene carriers for gene delivery. In vitro results revealed that the cytotoxicity of the multifunctional magnetic nanoparticles was lower compared to that of pristine. magnetic nanoparticles. Furthermore, we demonstrated the specific uptake of the magnetic nanoparticles modified with PF to KB cells using WI-38 cells as comparison by confocal microscopy. The PF-modified magnetic nanoparticles can potentially be :employed as theranostic nanoplatforms for targeted gene delivery to cancer cells and simultaneous magnetic resonance imaging.