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

EJNMMI Research
Elisabeth EppardFrank Rösch

Abstract

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. 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. 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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Citations

Mar 29, 2020·Journal of Labelled Compounds & Radiopharmaceuticals·Pallab Datta, Soumendranath Ray
Sep 29, 2018·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Ivis F Chaple, Suzanne E Lapi

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Methods Mentioned

BETA
light scattering
Fluorescence Correlation Spectroscopy
amidation
dissection

Software Mentioned

Teratomo 3D
PSS WinGPC Unity
pmod

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