Synthesis and radiolabeling of (111)In-core-cross linked polymeric micelle-octreotide for near-infrared fluoroscopy and single photon emission computed tomography imaging

Bioorg Med Chem Lett. 2014 Jun 15;24(12):2781-5. doi: 10.1016/j.bmcl.2014.03.050. Epub 2014 Mar 25.

Abstract

The objective of this study was the development of a dual-modality imaging device, namely (111)In-core-cross-linked polymeric micelle (CCPM)-octreotide, for neuroendocrine tumor detection, using near-infrared fluoroscopy (NIRF) and single photon emission computed tomography (SPECT). The tumor targeting ability of the (111)In-labeled CCPM-octreotide was evaluated in a tumor mouse model. SPECT/CT, NIRF and gamma imaging results showed high tumor uptake of (111)In-labeled CCPM-octreotide. In contrast, there was a much lower signal in the same mouse model injected with (111)In-labeled CCPM. The high accumulation of (111)In-labeled CCPM-octreotide in U87 tumor was reduced after co-injection with an excess amount of CCPM-octreotide. These results suggested CCPM-octreotide's potential applications in tumor diagnosis, drug delivery and molecular imaging.

Keywords: Dual-modality imaging; Near-infrared fluoroscopy; Octreotide; Single photon emission computed tomography; Tumor detection.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Intravenous
  • Animals
  • Cross-Linking Reagents / chemistry*
  • Diagnostic Imaging
  • Disease Models, Animal
  • Drug Delivery Systems
  • Fluoroscopy*
  • Mice
  • Micelles*
  • Microscopy, Electron, Transmission
  • Models, Molecular
  • Neoplasms / drug therapy
  • Octreotide / chemistry*
  • Polymers / chemistry*
  • Radiopharmaceuticals
  • Tomography, Emission-Computed, Single-Photon*

Substances

  • Cross-Linking Reagents
  • Micelles
  • Polymers
  • Radiopharmaceuticals
  • Octreotide