TSPO-targeted NIR-fluorescent ultra-small iron oxide nanoparticles for glioblastoma imaging

Nunzio Denora, Chaedong Lee, Rosa Maria Iacobazzi, Ji Young Choi, In Ho Song, Jung Sun Yoo, Yuanzhe Piao, Antonio Lopalco, Francesco Leonetti, Byung Chul Lee, Sang Eun Kim

Research output: Journal article publicationJournal articleAcademic researchpeer-review

8 Citations (Scopus)

Abstract

The translocator protein 18 kDa (TSPO) is mainly located in outer membrane of mitochondria and results highly expressed in a variety of tumor including breast, colon, prostate, ovarian and brain (such as glioblastoma). Glioblastoma multiforme (GBM) is the most common and lethal type of primary brain tumor. Although GBM patients had currently available therapies, the median survival is <14 months. Complete surgical resection of GBM is critical to improve GBM treatment. In this study, we performed the one-step synthesis of water-dispersible ultra-small iron oxide nanoparticles (USPIONs) and combine them with an imidazopyridine based TSPO ligand and a fluorescent dye. The optical and structural characteristics of TSPO targeted-USPIONs were properly evaluated at each step of preparation demonstrating the high colloidal stability in physiological media and the ability to preserve the relevant optical properties in the NIR region. The cellular uptake in TSPO expressing cells was assessed by confocal microscopy. The TSPO selectivity was confirmed in vivo by competition studies with the TSPO ligand PK 11195. In vivo fluorescence imaging of U87-MG xenograft models were performed to highlight the great potential of the new NIR imaging nanosystem for diagnosis and successful delineation of GBM.

Original languageEnglish
Article number105047
JournalEuropean Journal of Pharmaceutical Sciences
Volume139
Early online date15 Aug 2019
DOIs
Publication statusPublished - 1 Nov 2019

Keywords

  • Glioblastoma multiforme
  • Mitochondrial targeting
  • NIR imaging
  • TSPO
  • USPIONs

ASJC Scopus subject areas

  • Pharmaceutical Science

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