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

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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.

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Synthesis and in vivo fate of zwitterionic near-infrared fluorophores.

Sergey Alyabyev, Gabor Patonay, Khaled Nasr … (2011)

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Pamidronate prevents skeletal complications and is effective palliative treatment in women with breast carcinoma and osteolytic bone metastases: long term follow-up of two randomized, placebo-controlled trials.

Jimmy R. Theriault, J. Simeone, James D R Knight … (2000)

Pamidronate therapy previously has been shown to reduce skeletal complications effectively for up to 12 months in breast carcinoma patients with bone metastases. The current study data provide further follow-up results regarding the effects of long term (up to 24 months) pamidronate treatment in women with breast carcinoma and osteolytic metastases. Follow-up results from two prospective, multicenter, randomized, double-blind, placebo-controlled intervention trials conducted at academic and community oncology centers were combined to provide a large data set with which to evaluate the long term efficacy and safety of pamidronate therapy. Seven hundred fifty-four women with Stage IV breast carcinoma and osteolytic metastases were randomized to the 2 treatment arms of the trial. Three patients were excluded from the intent-to-treat population for the analysis. A total of 751 evaluable patients were randomized to receive either a 90-mg intravenous pamidronate infusion (367 patients) or a placebo infusion (384 patients) every 3-4 weeks. The primary outcome measures were skeletal morbidity rate (events/year), proportion of patients developing a skeletal complication, and time to first skeletal complication. Of the 367 women receiving pamidronate, 115 (31.3%) completed the trial and 81 (22.1%) discontinued the study due to adverse events. Of the 384 women who received placebo, 100 (26.0%) completed the study and 76 (19.8%) discontinued the study due to adverse events. The skeletal morbidity rate was 2.4 in the pamidronate group and 3.7 in the placebo group (P < 0.001). In the pamidronate group, 186 of the 367 patients (51%) had skeletal complications compared with 246 of the 384 patients in the placebo group (64%) (P < 0.001). The median time to first skeletal complication was 12.7 months in the pamidronate group and 7 months in the placebo group (P < 0.001). Six patients treated with pamidronate discontinued treatment due to drug-related adverse events. Pain and analgesic scores were significantly worse in the placebo group compared with those patients in the pamidronate group. In the current study, monthly infusions of 90 mg of pamidronate as a supplement to antineoplastic therapy were found to be well tolerated and superior to antineoplastic therapy alone in preventing skeletal complications and palliating symptoms for at least 24 months in breast carcinoma patients with osteolytic bone metastases. Copyright 2000 American Cancer Society.

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In vivo near-infrared fluorescence imaging of osteoblastic activity.

R Lenkinski, OMAR MAHMOOD, John V. Frangioni … (2001)

In vertebrates, the development and integrity of the skeleton requires hydroxyapatite (HA) deposition by osteoblasts. HA deposition is also a marker of, or a participant in, processes as diverse as cancer and atherosclerosis. At present, sites of osteoblastic activity can only be imaged in vivo using gamma-emitting radioisotopes. The scan times required are long, and the resultant radioscintigraphic images suffer from relatively low resolution. We have synthesized a near-infrared (NIR) fluorescent bisphosphonate derivative that exhibits rapid and specific binding to HA in vitro and in vivo. We demonstrate NIR light-based detection of osteoblastic activity in the living animal, and discuss how this technology can be used to study skeletal development, osteoblastic metastasis, coronary atherosclerosis, and other human diseases.

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Author and article information

Journal

Journal ID (nlm-ta): Theranostics

Journal ID (iso-abbrev): Theranostics

Journal ID (publisher-id): thno

Title: Theranostics

Publisher: Ivyspring International Publisher (Sydney )

ISSN (Electronic): 1838-7640

Publication date Collection: 2015

Publication date (Electronic): 1 March 2015

Volume: 5

Issue: 6

Pages: 609-617

Affiliations

1. Division of Hematology/Oncology, Department of Medicine, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, MA 02215;

2. Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, China, 110016;

3. Advanced Imaging Research Center, The University of Texas Southwestern Medical Center, Dallas, TX 75390;

4. Department of Biomedical Engineering, OHSU Center for Spatial Systems Biology, Knight Cancer Institute, Oregon Health & Science University, Portland, OR 97201.

Author notes

✉ Corresponding authors: Summer L. Gibbs, Ph.D. Collaborative Life Sciences Building, 2730 SW Moody Ave, Mail Code: CL3SG, Portland, OR 97201. Office: 503-494-8940; Fax: 503-418-9311 Email: gibbss@ 123456ohsu.edu or Hak Soo Choi, Ph.D. 330 Brookline Ave. Room SL-436A, Boston, MA 02215. Office: 617-667-6024; Fax: 617-667-0214 Email: hchoi@ 123456bidmc.harvard.edu .

^*These authors contributed equally to this work.

Competing Interests: The authors have declared that no competing interest exists.

Article

Publisher ID: thnov05p0609

DOI: 10.7150/thno.11222

PMC ID: 4377729

PubMed ID: 25825600

SO-VID: 5942d74e-7e3b-4fe5-9d41-c3194137af7e

Copyright © © 2015 Ivyspring International Publisher. Reproduction is permitted for personal, noncommercial use, provided that the article is in whole, unmodified, and properly cited. See http://ivyspring.com/terms for terms and conditions.

History

Date received : 2 December 2014

Date accepted : 23 January 2015

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

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Most cited references 31

Synthesis and in vivo fate of zwitterionic near-infrared fluorophores.

Pamidronate prevents skeletal complications and is effective palliative treatment in women with breast carcinoma and osteolytic bone metastases: long term follow-up of two randomized, placebo-controlled trials.

In vivo near-infrared fluorescence imaging of osteoblastic activity.

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Cited by 18

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