Surface modification of PLGA nanospheres with Gd-DTPA and Gd-DOTA for high-relaxivity MRI contrast agents

Author(s)
Gerda Ratzinger-Stöger, Prashant Agrawal, Wilfried Körner, Julia Lonkai, Honorius M. H. F. Sanders, Enzo Terreno, Michael Wirth, Gustav J. Strijkers, Klaas Nicolay, Franz Gabor
Abstract

The preparation of particulate contrast agents for magnetic resonance imaging (MRI) based on biodegradable poly(D,L-lactide-co-glycolide) (PLGA) nanocarriers is reported. By spacer-aided covalent surface-grafting of the prominent chelating ligands diethylenetriaminepentaacetic acid (DTPA) and 1,4,7, 10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), respectively, up to 236 mu g gadolinium per mg PLGA can be immobilized in a stable manner. Due to the localisation at the particle surface, water protons may effectively interact with the gadolinium chelates and the modified particles exhibit high proton relaxivities as confirmed by T1 relaxivities of up to 17.5 mM(-1)s(-1) (25 degrees C, 1.41 T) in case of Gd-DOTA-functionalized carriers and also supported by NMRD profiles. The obtained values compare favorably with marketed low-molecular weight contrast agents and thus suggest suitability for in vivo use. (C) 2010 Elsevier Ltd. All rights reserved.

Organisation(s)
External organisation(s)
Eindhoven University of Technology, University of Turin
Journal
Biomaterials
Volume
31
Pages
8716-8723
No. of pages
8
ISSN
0142-9612
DOI
https://doi.org/10.1016/j.biomaterials.2010.07.095
Publication date
2010
Peer reviewed
Yes
Austrian Fields of Science 2012
3012 Pharmacy, Pharmacology, Toxicology
Portal url
https://ucrisportal.univie.ac.at/en/publications/4fff783a-b381-4a27-be50-a014ea3bddfe