Enhanced cell uptake of superparamagnetic iron oxide nanoparticles through direct chemisorption of FITC-Tat-PEG600-b-poly(glycerol monoacrylate)

Magnetic nanoparticles (MNPs) functionalized with specific ligands are emerging as a highly integrated platform for cancer targeting, drug delivery, and magnetic resonance imaging applications. In this study, we describe a multifunctional magnetic nanoparticle system (FITC-Tat MNPs) consisting of a fluorescently labeled cell penetrating peptide (FITC-Tat peptide), a biocompatible block copolymer PEG(600)-b-poly(glycerol monoacrylate) (PEG(600)-b-PGA), and a superparamagnetic iron oxide (SPIO) nanoparticle core. The particles were prepared by direct chemisorption of PEG(600)-b-PGA conjugated with FITC-Tat peptide on the SPIO nanoparticles. FITC-MNPs without Tat were prepared for comparison. Flow cytometry assays revealed significantly higher uptake of FITC-Tat MNPs compared to FITC-MNPs in Caco-2 cells. These results were confirmed using confocal laser scanning microscopy (LSCM), which further demonstrated that the FITC-Tat MNPs accumulated in the cytoplasm and nucleus while the FITC-MNPs were localized in the cell membrane compartments. The FITC-Tat MNPs did not exhibit observable cytotoxicity in MTS assays. (C) 2012 Elsevier B. V. All rights reserved.