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


K. Bao, K. A. Nasr, H. Hyun, J. H. Lee, J. Gravier, S. L. Gibbs, and H. S. Choi. 2015. “Charge and hydrophobicity effects of NIR fluorophores on bone-specific imaging.” Theranostics, 5, Pp. 609-17.


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.


Bao, KaiNasr, Khaled AHyun, HoonLee, Jeong HeonGravier, JulienGibbs, Summer LChoi, Hak SooengR01 EB011523/EB/NIBIB NIH HHS/R01-EB-011523/EB/NIBIB NIH HHS/Research Support, N.I.H., ExtramuralAustraliaTheranostics. 2015 Mar 1;5(6):609-17. doi: 10.7150/thno.11222. eCollection 2015.