TY - JOUR
T1 - Surface modification of PLGA nanospheres with Gd-DTPA and Gd-DOTA for high-relaxivity MRI contrast agents
AU - Ratzinger, G.
AU - Agrawal, P.
AU - Koerner, W.
AU - Lonkai, J.
AU - Sanders, H.M.H.F.
AU - Terreno, E.
AU - Wirth, M.
AU - Strijkers, G. J.
AU - Nicolay, K.
AU - Gabor, F.
PY - 2010/11
Y1 - 2010/11
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 μg 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−1s−1 (25 °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.
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 μg 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−1s−1 (25 °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.
KW - Nanoparticle
KW - MRI (magnetic resonance imaging)
KW - Surface modification
KW - Poly(D,L-lactide-co-glycolide)
KW - Gadolinium
KW - Chelate
U2 - 10.1016/j.biomaterials.2010.07.095
DO - 10.1016/j.biomaterials.2010.07.095
M3 - Article
C2 - 20797782
SN - 0142-9612
VL - 31
SP - 8716
EP - 8723
JO - Biomaterials
JF - Biomaterials
IS - 33
ER -