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A bisphosphonate for ¹⁹F-magnetic resonance imaging.

ABSTRACT: ¹⁹F-magnetic resonance imaging (MRI) is a promising technique that may allow us to measure the concentration of exogenous fluorinated imaging probes quantitatively in vivo. Here, we describe the synthesis and characterisation of a novel geminal bisphosphonate (¹⁹F-BP) that contains chemically-equivalent fluorine atoms that show a single and narrow ¹⁹F resonance and a bisphosphonate group that may be used for labelling inorganic materials based in calcium phosphates and metal oxides. The potential of ¹⁹F-BP to provide contrast was analysed in vitro and in vivo using ¹⁹F-MRI. In vitro studies demonstrated the potential of ¹⁹F-BP as an MRI contrast agent in the millimolar concentration range with signal-to-noise ratios (SNR) comparable to previously reported fluorinated probes. The preliminary in vivo MRI study reported here allowed us to visualise the biodistribution of ¹⁹F-BP, showing uptake in the liver and in the bladder/urinary system areas. However, bone uptake was not observed. In addition, ¹⁹F-BP showed undesirable toxicity effects in mice that prevent further studies with this compound at the required concentrations for MRI contrast. This study highlights the importance of developing ¹⁹F MRI probes with the highest signal intensity achievable.

SUBMITTER: Kenny GD

PROVIDER: S-EPMC4834630 | biostudies-literature | 2016 Apr

REPOSITORIES: biostudies-literature

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A bisphosphonate for 19F-magnetic resonance imaging.

Kenny Gavin D GD Shaw Karen P KP Sivachelvam Saranja S White Andrew J P AJ Botnar Rene M RM Botnar Rene M RM T M de Rosales Rafael R

Journal of fluorine chemistry 20160401

19F-magnetic resonance imaging (MRI) is a promising technique that may allow us to measure the concentration of exogenous fluorinated imaging probes quantitatively in vivo. Here, we describe the synthesis and characterisation of a novel geminal bisphosphonate (19F-BP) that contains chemically-equivalent fluorine atoms that show a single and narrow 19F resonance and a bisphosphonate group that may be used for labelling inorganic materials based in calcium p ...[more]

PMID: 27110036

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Project description:BackgroundMacrophages play a pivotal role in vascular inflammation and predict cardiovascular complications. Fluorine-19 magnetic resonance imaging (19F MRI) with intravenously applied perfluorocarbon allows a background-free direct quantification of macrophage abundance in experimental vascular disease models in mice. Recently, perfluorooctyl bromide-nanoemulsion (PFOB-NE) was applied to effectively image macrophage infiltration in a pig model of myocardial infarction using clinical MRI scanners. In the present proof-of-concept approach, we aimed to non-invasively image monocyte/macrophage infiltration in response to carotid artery angioplasty in pigs using 19F MRI to assess early inflammatory response to mechanical injury.MethodsIn eight minipigs, two different types of vascular injury were conducted: a mild injury employing balloon oversize angioplasty only (BA, n = 4) and a severe injury provoked by BA in combination with endothelial denudation (BA + ECDN, n = 4). PFOB-NE was administered intravenously three days after injury followed by 1H and 19F MRI to assess vascular inflammatory burden at day six. Vascular response to mechanical injury was validated using X-ray angiography, intravascular ultrasound and immunohistology in at least 10 segments per carotid artery.ResultsAngioplasty was successfully induced in all eight pigs. Response to injury was characterized by positive remodeling with predominantly adventitial wall thickening and concomitant infiltration of monocytes/macrophages. No severe adverse reactions were observed following PFOB-NE administration. In vivo 19F signals were only detected in the four pigs following BA + ECDN with a robust signal-to-noise ratio (SNR) of 14.7 ± 4.8. Ex vivo analysis revealed a linear correlation of 19F SNR to local monocyte/macrophage cell density. Minimum detection limit of infiltrated monocytes/macrophages was estimated at approximately 410 cells/mm2.ConclusionsIn this proof-of-concept study, 19F MRI enabled quantification of monocyte/macrophage infiltration after vascular injury with sufficient sensitivity. This may provide the opportunity to non-invasively monitor vascular inflammation with MRI in patients after angioplasty or even in atherosclerotic plaques.

Dataset Information

A bisphosphonate for ¹⁹F-magnetic resonance imaging.

Publications

A bisphosphonate for <sup>19</sup>F-magnetic resonance imaging.

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