Design, synthesis and in vitro characterization of fluorescent and paramagnetic CXCR4-targeted imaging agents

Ole Tietz, Nazila Kamaly, Graham Smith, Elham Shamsaei, Kishore K. Bhakoo, Nicholas J. Long, Eric O. Aboagye

Research output: Contribution to journalJournal articleResearchpeer-review

Abstract

The G-protein coupled C-X-C chemokine receptor type 4 (CXCR4) is highly overexpressed in a range of cancers and is therefore an excellent biomarker for cancer imaging. To this end targeted iron oxide nanoparticles were developed and utilised for in vitro imaging of MDA-MB-231 breast cancer cells overexpressing the CXCR4 receptor. Nanoparticles comprising an iron oxide core, encapsulated in a stabilising epichlorohydrin crossed-linked dextran polymer, were conjugated to a cyclopentapeptide with affinity to the CXCR4 receptor. The particles were characterized for their size, surface charge and r2 relaxivity at 4.7 T. MR imaging of the CXCR4 receptor with targeted iron oxide nanoparticles revealed an approximately 3-fold increase in T2 signal enhancement of MDA-MB-231 cells compared to non-targeted controls. Prussian blue staining of labeled MDA-MB-231 cells revealed darker and more intense staining of the cellular membrane. This study demonstrates the potential of targeted iron oxide nanoparticles for the imaging of the CXCR4 receptor by magnetic resonance imaging (MRI).
Original languageEnglish
JournalAmerican Journal of Nuclear Medicine and Molecular Imaging
Volume3
Issue number4
Pages (from-to)372-383
ISSN2160-8407
Publication statusPublished - 2013
Externally publishedYes

Keywords

  • CXCR4
  • Iron oxide nanoparticles
  • Tumor MRI
  • Targeted nanoparticles
  • T2 imaging
  • Cyclopentapeptide

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