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

Details

Serval ID
serval:BIB_2D88ACBFD811
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
Pharmacokinetics and biodistribution study of self-assembled Gd-micelles demonstrating blood-pool contrast enhancement for MRI.
Journal
International journal of pharmaceutics
Author(s)
Vorobiev V., Babič A., Crowe L.A., Van De Looij Y., Lenglet S., Thomas A., Helm L., Vallée J.P., Allémann E.
ISSN
1873-3476 (Electronic)
ISSN-L
0378-5173
Publication state
Published
Issued date
10/09/2019
Peer-reviewed
Oui
Volume
568
Pages
118496
Language
english
Notes
Publication types: Journal Article
Publication Status: ppublish
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. Gd-micelles 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
Animals, Cell Survival/drug effects, Contrast Media/administration & dosage, Contrast Media/pharmacokinetics, Gadolinium/administration & dosage, Gadolinium/pharmacokinetics, Heterocyclic Compounds/administration & dosage, Heterocyclic Compounds/pharmacokinetics, Humans, MCF-7 Cells, Magnetic Resonance Imaging, Male, Mice, Inbred BALB C, Micelles, Organometallic Compounds/administration & dosage, Organometallic Compounds/pharmacokinetics, Tissue Distribution, Blood pool contrast agents, Gd-DOTA, Gd-micelles, Magnetic resonance angiography, Pharmacokinetics
Pubmed
Web of science
Create date
23/07/2019 9:00
Last modification date
30/01/2020 7:20
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