TY - JOUR
T1 - Surface modification of PLGA nanospheres with Gd-DTPA and Gd-DOTA for high-relaxivity MRI contrast agents
AU - Ratzinger-Stöger, Gerda
AU - Agrawal, Prashant
AU - Körner, Wilfried
AU - Lonkai, Julia
AU - Sanders, Honorius M. H. F.
AU - Terreno, Enzo
AU - Wirth, Michael
AU - Strijkers, Gustav J.
AU - Nicolay, Klaas
AU - Gabor, Franz
PY - 2010
Y1 - 2010
N2 - 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.
AB - 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.
U2 - 10.1016/j.biomaterials.2010.07.095
DO - 10.1016/j.biomaterials.2010.07.095
M3 - Article
SN - 0142-9612
VL - 31
SP - 8716
EP - 8723
JO - Biomaterials
JF - Biomaterials
IS - 33
ER -