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Title

Pharmacokinetics and biodistribution study of self-assembled Gd-micelles demonstrating blood-pool contrast enhancement for MRI

Authors
Helm, Lothar
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Published in International Journal of Pharmaceutics. 2019, vol. 568, p. 118496
Abstract Magnetic resonance angiography (MRA) requires the use of contrast agents (CAs) to enable accurate diagnosis. There are currently no CAs on the market with appropriate pharmacokinetic (PK) parameters, namely long persistence in the blood, that can be easily used for MRA. We have recently synthesized amphiphilic building blocks loaded with gadolinium (Gd), which self-assemble into Gd-micelles in aqueous media, and have evaluated their potential as a blood-pool contrast agent (BPCA) in vivo. To assess the short and long term PK of Gd-micelles, the blood and organs of the mice were analyzed at t=30 min, 1, 2, 3 h, 7, 14 and 21 days. Gd-DOTA was used as a control because it is the gold-standard CA for MRA despite its rapid clearance from the blood compartment. Gdmicelles circulated in the blood for more than 3 h postinjection whereas Gd-DOTA was eliminated less than half an hour postinjection. No side effects were observed in the mice up to the end of the study at 21 days and no accumulation of Gd was observed in the brain or bones. The Magnetic Resonance Imaging (MRI) parameters and the results of this in vivo study indicate the true BCPA properties of Gd-micelles and warrant further development.
Keywords Magnetic resonance angiographyBlood pool contrast agentsGd-micellesGd-DOTAPharmacokinetics
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PMID: 31279053
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Research groups Technologie pharmaceutique
Imagerie cardiaque fonctionnelle (541)
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VOROBIEV, Vassily et al. Pharmacokinetics and biodistribution study of self-assembled Gd-micelles demonstrating blood-pool contrast enhancement for MRI. In: International Journal of Pharmaceutics, 2019, vol. 568, p. 118496. doi: 10.1016/j.ijpharm.2019.118496 https://archive-ouverte.unige.ch/unige:126345

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Deposited on : 2019-11-15

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