4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 12, Pages 2781-2785

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.03.050

Keywords

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

Funding

  1. National Natural Science Foundation of China [81071198, 81172082, 81371592]
  2. Beijing Natural Science Foundation [7132040]

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The objective of this study was the development of a dual-modality imaging device, namely In-111-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 In-111-labeled CCPM-octreotide was evaluated in a tumor mouse model. SPECT/CT, NIRF and gamma imaging results showed high tumor uptake of In-111-labeled CCPM-octreotide. In contrast, there was a much lower signal in the same mouse model injected with In-111-labeled CCPM. The high accumulation of In-111-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. (C) 2014 Elsevier Ltd. All rights reserved.

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