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

Gerda Ratzinger; Prashant Agrawal; Wilfried Körner; Julia Lonkai; Honorius M. H. F. Sanders; Enzo Terreno; Michael Wirth; Gustav J. Strijkers; Klaas Nicolay; Franz Gabor

doi:https://doi.org/10.1016/j.biomaterials.2010.07.095

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

Gerda Ratzinger, Prashant Agrawal, Wilfried Körner, Julia Lonkai, Honorius M. H. F. Sanders, Enzo Terreno, Michael Wirth, Gustav J. Strijkers, Klaas Nicolay, Franz Gabor

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Research output: Contribution to journal › Article › Academic › peer-review

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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 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(-1)s(-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

Original language	English
Pages (from-to)	8716-8723
Journal	Biomaterials
Volume	31
Issue number	33
DOIs	https://doi.org/10.1016/j.biomaterials.2010.07.095
Publication status	Published - 2010

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https://doi.org/10.1016/j.biomaterials.2010.07.095

Cite this

@article{7440c473f8004b04a3ccd49c41ec7c61,

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

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 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(-1)s(-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",

author = "Gerda Ratzinger and Prashant Agrawal and Wilfried K{\"o}rner and Julia Lonkai and Sanders, {Honorius M. H. F.} and Enzo Terreno and Michael Wirth and Strijkers, {Gustav J.} and Klaas Nicolay and Franz Gabor",

year = "2010",

doi = "https://doi.org/10.1016/j.biomaterials.2010.07.095",

language = "English",

volume = "31",

pages = "8716--8723",

journal = "Biomaterials",

issn = "0142-9612",

publisher = "Elsevier BV",

number = "33",

}

TY - JOUR

T1 - Surface modification of PLGA nanospheres with Gd-DTPA and Gd-DOTA for high-relaxivity MRI contrast agents

AU - Ratzinger, 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 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(-1)s(-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(-1)s(-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

U2 - https://doi.org/10.1016/j.biomaterials.2010.07.095

DO - https://doi.org/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 -