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Authors: Eppard, Elisabeth
Fuente, Ana de la
Mohr, Nicole
Allmeroth, Mareli
Zentel, Rudolf
Miederer, Matthias
Pektor, Stefanie
Rösch, Frank
Title: Labeling of DOTA-conjugated HPMA-based polymers with trivalent metallic radionuclides for molecular imaging
Online publication date: 2-Aug-2018
Language: english
Abstract: Background In this work, the in vitro and in vivo stabilities and the pharmacology of HPMA-made homopolymers were studied by means of radiometal-labeled derivatives. Aiming to identify the fewer amount and the optimal DOTA-linker structure that provides quantitative labeling yields, diverse DOTA-linker systems were conjugated in different amounts to HPMA homopolymers to coordinate trivalent radiometals Me(III)* = gallium-68, scandium-44, and lutetium-177. Results Short linkers and as low as 1.6% DOTA were enough to obtain labeling yields > 90%. Alkoxy linkers generally exhibited lower labeling yields than alkane analogues despite of similar chain length and DOTA incorporation rate. High stability of the radiolabel in all examined solutions was observed for all conjugates. Labeling with scandium-44 allowed for in vivo PET imaging and ex vivo measurements of organ distribution for up to 24 h. Conclusions This study confirms the principle applicability of DOTA-HPMA conjugates for labeling with different trivalent metallic radionuclides allowing for diagnosis and therapy.
DDC: 610 Medizin
610 Medical sciences
Institution: Johannes Gutenberg-Universität Mainz
Department: FB 09 Chemie, Pharmazie u. Geowissensch.
FB 04 Medizin
Place: Mainz
Version: Published version
Publication type: Zeitschriftenaufsatz
License: CC-BY
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Journal: EJNMMI Research
Pages or article number: Art. 16
Publisher: Springer
Publisher place: Berlin
Issue date: 2018
ISSN: 2191-219X
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Appears in collections:JGU-Publikationen

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