Charge and hydrophobicity effects of NIR fluorophores on bone-specific imaging

Kai Bao, Khaled A. Nasr, Hoon Hyun, Jeong Heon Lee, Julien Gravier, Summer L. Gibbs, Hak Soo Choi

Research output: Contribution to journalArticlepeer-review

42 Scopus citations

Abstract

Recent advances in near-infrared (NIR) fluorescence imaging enabled real-time intraoperative detection of bone metastases, bone growth, and tissue microcalcification. Pamidronate (PAM) has been widely used for this purpose because of its high binding affinity toward bone and remarkable therapeutic effects. Herein we describe the development of a series of PAM-conjugated NIR fluorophores that varied in net charges and hydrophobicity, and compared their bone targeting efficiency, biodistribution, and blood clearance. Since the targeting moiety, PAM, is highly negatively charged but small, the overall in vivo bone targeting and biodistribution were mediated by the physicochemical properties of conjugated fluorophores.

Original languageEnglish (US)
Pages (from-to)609-617
Number of pages9
JournalTheranostics
Volume5
Issue number6
DOIs
StatePublished - 2015

Keywords

  • Bone targeting
  • Charge and hydrophobicity
  • Microcalcification
  • Near-infrared fluorophores
  • Zwitterionic fluorophores

ASJC Scopus subject areas

  • Medicine (miscellaneous)
  • Pharmacology, Toxicology and Pharmaceutics (miscellaneous)

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