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

Charge and hydrophobicity effects of NIR fluorophores on bone-specific imaging.
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DOI:
10.7150/thno.11222
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发表时间:
2015
期刊:
影响因子:
12.4
通讯作者:
Choi HS
Choi HS
中科院分区:
医学1区
文献类型:
--
作者:
Bao K;Nasr KA;Hyun H;Lee JH;Gravier J;Gibbs SL;Choi HS

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近红外(NIR)荧光成像的最新进展使术中实时检测骨转移、骨生长和组织微钙化成为可能。帕米膦酸盐(PAM)因其与骨的高亲和力和显著的治疗效果而被广泛用于这一目的。在这里,我们描述了一系列PAM共轭近红外荧光团的发展,不同的净电荷和疏水性,并比较其骨靶向效率,生物分布和血液清除。由于靶向部分,PAM,是高度负电荷,但小,整体体内骨靶向和生物分布介导的共轭荧光团的物理化学性质。
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.
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