68Ga-radiolabeled AGuIX nanoparticles as dual-modality imaging agents for PET/MRI-guided radiation therapy

Nanomedicine (Lond). 2017 Jul;12(13):1561-1574. doi: 10.2217/nnm-2017-0032. Epub 2017 Jun 16.

Abstract

Aim: The aim of this study was to develop a dual-modality positron emission tomography/magnetic resonance (PET/MR) imaging probe by radiolabeling gadolinium-containing AGuIX derivatives with the positron-emitter Gallium-68 (68Ga).

Materials & methods: AGuIX@NODAGA nanoparticles were labeled with 68Ga at high efficiency. Tumor accumulation in an appropriate disease model was assessed by ex vivo biodistribution and in vivo PET/MR imaging.

Results: 68Ga-AGuIX@NODAGA was proven to passively accumulate in U87MG human glioblastoma tumor xenografts. Metabolite assessment in serum, urine and tumor samples showed that 68Ga-AGuIX@NODAGA remains unmetabolized up to at least 60 min postinjection.

Conclusion: This study demonstrates that 68Ga-AGuIX@NODAGA can be used as a dual-modality PET/MR imaging agent with passive accumulation in the diseased area, thus showing great potential for PET/MR image-guided radiation therapy.

Keywords: Gallium-68; PET/MR imaging; ultrasmall AGuIX nanoparticles.

MeSH terms

  • Acetates / chemistry*
  • Animals
  • Cell Line, Tumor
  • Central Nervous System Neoplasms / diagnostic imaging*
  • Central Nervous System Neoplasms / radiotherapy
  • Chromatography, High Pressure Liquid
  • Contrast Media / chemistry*
  • Coordination Complexes / chemistry*
  • Female
  • Gallium Radioisotopes / blood
  • Gallium Radioisotopes / chemistry*
  • Gallium Radioisotopes / urine
  • Glioblastoma / diagnostic imaging*
  • Glioblastoma / radiotherapy
  • Heterocyclic Compounds, 1-Ring / chemistry*
  • Humans
  • Magnetic Resonance Imaging / methods
  • Mice
  • Mice, SCID
  • Nanoparticles / chemistry*
  • Positron-Emission Tomography / methods
  • Siloxanes / chemistry*
  • Tissue Distribution

Substances

  • 1-(1,3-carboxypropyl)-4,7-carboxymethyl-1,4,7-triazacyclononane
  • Acetates
  • Contrast Media
  • Coordination Complexes
  • Gallium Radioisotopes
  • Heterocyclic Compounds, 1-Ring
  • Siloxanes