DOI: 10.1186/s13550-018-0372-xPages: 1-14

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

1. University Medical Center Bonn, Clinic for Nuclear Medicine

2. Johannes Gutenberg University Mainz, Institute of Nuclear Chemistry

3. Johannes Gutenberg University Mainz, Institute of Organic Chemistry

4. University Medical Center Mainz, Clinic for Nuclear Medicine

Correspondence to:
Stefanie Pektor
Tel: +49 6131 17 2868
Email: Stefanie.pektor@unimedizin-mainz.de

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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.

This article is freely available, click here to access the full text/PDF

  • Accepted: Feb 19, 2018
  • Online: Feb 27, 2018

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