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Effective PEGylation of Iron Oxide Nanoparticles for High Performance In Vivo Cancer Imaging

Authors

  • Dongfang Liu,

    1. Jiangsu Key Laboratory for Biomaterials and Devices, State Key Laboratory of Bioelectronics, School of Biological Science and Medical Engineering, Southeast University, Nanjing 210096, China
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  • Wei Wu,

    1. Laboratory of Mesoscopic Chemistry and Department of Polymer, Science & Engineering, College of Chemistry & Chemical Engineering, Nanjing University, Nanjing 210093, China
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  • Jingjing Ling,

    1. Jiangsu Key Laboratory for Biomaterials and Devices, State Key Laboratory of Bioelectronics, School of Biological Science and Medical Engineering, Southeast University, Nanjing 210096, China
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  • Song Wen,

    1. Laboratory of Molecular Imaging, School of Medicine, Southeast University, Nanjing 210096, China
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  • Ning Gu,

    Corresponding author
    1. Jiangsu Key Laboratory for Biomaterials and Devices, State Key Laboratory of Bioelectronics, School of Biological Science and Medical Engineering, Southeast University, Nanjing 210096, China
    • Jiangsu Key Laboratory for Biomaterials and Devices, State Key Laboratory of Bioelectronics, School of Biological Science and Medical Engineering, Southeast University, Nanjing 210096, China.
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  • Xizhi Zhang

    1. Jiangsu Key Laboratory for Biomaterials and Devices, State Key Laboratory of Bioelectronics, School of Biological Science and Medical Engineering, Southeast University, Nanjing 210096, China
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Abstract

A practical and effective strategy for synthesizing PEGylated superparamagnetic iron oxide nanoparticles (SPIONs) is established. In this strategy, poly(acrylic acid) (PAA) is combined with SPIONs via multiple coordination between the carboxylic groups of PAA and SPIONs, which introduces abundant carboxylic groups, then, α,ω-diamino PEG is linked to SPIONs via the amidation of the carboxylic groups. The synthesized PEGylated SPIONs exhibit no cytotoxicity and high resistance to phagocytosis by macrophages in vitro as well as low uptake by the liver and spleen in vivo, which makes the SPIONs highly efficient in tumor imaging by magnetic resonance imaging (MRI) at a relatively low dose of SPIONs. These outstanding properties are largely due to the significant shielding effect of the dense PEG coating as well as the net neutral surface of the PEGylated SPIONs in physiological conditions. In summary, the PEGylated SPIONs prepared by this strategy exhibit great application potential in tumor imaging as MRI contrast agents targeting through enhanced permeability and retention (EPR) effect.

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