Charge and Hydrophobicity Effects of NIR Fluorophores on Bone-Specific Imaging

被引：46

作者：

Bao, Kai ^{[1
,2
,3
]}

Nasr, Khaled A. ^{[1
,2
,4
]}

Hyun, Hoon ^{[1
,2
]}

Lee, Jeong Heon ^{[1
,2
]}

Gravier, Julien ^{[1
,2
]}

Gibbs, Summer L. ^{[5
]}

Choi, Hak Soo ^{[1
,2
]}

机构：

[1] Beth Israel Deaconess Med Ctr, Dept Med, Div Hematol Oncol, Boston, MA 02215 USA

[2] Harvard Univ, Sch Med, Boston, MA 02215 USA

[3] Shenyang Pharmaceut Univ, Minist Educ, Key Lab Struct Based Drug Design & Discovery, Shenyang 110016, Peoples R China

[4] Univ Texas SW Med Ctr Dallas, Adv Imaging Res Ctr, Dallas, TX 75390 USA

[5] Oregon Hlth & Sci Univ, Knight Canc Inst, Ctr Spatial Syst Biol, Dept Biomed Engn, Portland, OR 97201 USA

来源：

THERANOSTICS | 2015年 / 5卷 / 06期

关键词：

Near-infrared fluorophores; Bone targeting; Charge and hydrophobicity; Microcalcification; Zwitterionic fluorophores; NEAR-INFRARED FLUOROPHORES; REAL-TIME; BISPHOSPHONATES; HYDROXYAPATITE; IDENTIFICATION; NANOPARTICLES; PALLIATION; PERFUSION; BINDING; PAIN;

D O I：

10.7150/thno.11222

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

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.

引用

收藏

页码：609 / 617

页数：9

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