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EJNMMI Research
Published in: EJNMMI Research 1/2018

Open Access 01-12-2018 | Original research

Labeling of DOTA-conjugated HPMA-based polymers with trivalent metallic radionuclides for molecular imaging

Authors: Elisabeth Eppard, Ana de la Fuente, Nicole Mohr, Mareli Allmeroth, Rudolf Zentel, Matthias Miederer, Stefanie Pektor, Frank Rösch

Published in: EJNMMI Research | Issue 1/2018

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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.
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Metadata
Title
Labeling of DOTA-conjugated HPMA-based polymers with trivalent metallic radionuclides for molecular imaging
Authors
Elisabeth Eppard
Ana de la Fuente
Nicole Mohr
Mareli Allmeroth
Rudolf Zentel
Matthias Miederer
Stefanie Pektor
Frank Rösch
Publication date
01-12-2018
Publisher
Springer Berlin Heidelberg
Published in
EJNMMI Research / Issue 1/2018
Electronic ISSN: 2191-219X
DOI
https://doi.org/10.1186/s13550-018-0372-x

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