RGD-functionalized ultrasmall iron oxide nanoparticles for targeted T1-weighted MR imaging of gliomas

Yu Luo; Jia Yang; Yu Yan; Jingchao Li; Mingwu Shen; Guixiang Zhang; Serge Mignani; Xiangyang Shi

doi:10.1039/C5NR04003E

RGD-functionalized ultrasmall iron oxide nanoparticles for targeted T₁-weighted MR imaging of gliomas†

Yu Luo,‡^a Jia Yang,‡^b Yu Yan,^a Jingchao Li,^a Mingwu Shen,*^a Guixiang Zhang,*^b Serge Mignani^c and Xiangyang Shi*^a

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* Corresponding authors

^a College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai 201620, People's Republic of China
E-mail: xshi@dhu.edu.cn, mwshen@dhu.edu.cn

^b Department of Radiology, Shanghai General Hospital, School of Medicine, Shanghai Jiaotong University, Shanghai 200080, People's Republic of China
E-mail: guixiangzhang@sina.com

^c Université Paris Descartes, PRES Sorbonne Paris Cité, CNRS UMR 860, Laboratoire de Chimie et de Biochimie pharmacologiques et toxicologique, 45, rue des Saints Pères, 75006 Paris, France

Abstract

We report a convenient approach to prepare ultrasmall Fe₃O₄ nanoparticles (NPs) functionalized with an arginylglycylaspartic acid (RGD) peptide for in vitro and in vivo magnetic resonance (MR) imaging of gliomas. In our work, stable sodium citrate-stabilized Fe₃O₄ NPs were prepared by a solvothermal route. Then, the carboxylated Fe₃O₄ NPs stabilized with sodium citrate were conjugated with polyethylene glycol (PEG)-linked RGD. The formed ultrasmall RGD-functionalized nanoprobe (Fe₃O₄-PEG-RGD) was fully characterized using different techniques. We show that these Fe₃O₄-PEG-RGD particles with a size of 2.7 nm are water-dispersible, stable, cytocompatible and hemocompatible in a given concentration range, and display targeting specificity to glioma cells overexpressing α_vβ₃ integrin in vitro. With the relatively high r₁ relaxivity (r₁ = 1.4 mM⁻¹ s⁻¹), the Fe₃O₄-PEG-RGD particles can be used as an efficient nanoprobe for targeted T₁-weighted positive MR imaging of glioma cells in vitro and the xenografted tumor model in vivo via an active RGD-mediated targeting pathway. The developed RGD-functionalized Fe₃O₄ NPs may hold great promise to be used as a nanoprobe for targeted T₁-weighted MR imaging of different α_vβ₃ integrin-overexpressing cancer cells or biological systems.

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Article information

DOI: https://doi.org/10.1039/C5NR04003E
Article type: Paper
Submitted: 17 Jun 2015
Accepted: 28 Jul 2015
First published: 31 Jul 2015

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Nanoscale, 2015,7, 14538-14546

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RGD-functionalized ultrasmall iron oxide nanoparticles for targeted T₁-weighted MR imaging of gliomas

Y. Luo, J. Yang, Y. Yan, J. Li, M. Shen, G. Zhang, S. Mignani and X. Shi, Nanoscale, 2015, 7, 14538 DOI: 10.1039/C5NR04003E

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