Autoren:	Eppard, Elisabeth Fuente, Ana de la Mohr, Nicole Allmeroth, Mareli Zentel, Rudolf Miederer, Matthias Pektor, Stefanie Rösch, Frank
Titel:	Labeling of DOTA-conjugated HPMA-based polymers with trivalent metallic radionuclides for molecular imaging
Online-Publikationsdatum:	2-Aug-2018
Erscheinungsdatum:	2018
Sprache des Dokuments:	Englisch
Zusammenfassung/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-Sachgruppe:	610 Medizin 610 Medical sciences
Veröffentlichende Institution:	Johannes Gutenberg-Universität Mainz
Organisationseinheit:	FB 09 Chemie, Pharmazie u. Geowissensch. FB 04 Medizin
Veröffentlichungsort:	Mainz
ROR:	https://ror.org/023b0x485
DOI:	http://doi.org/10.25358/openscience-800
URN:	urn:nbn:de:hebis:77-publ-584092
Version:	Published version
Publikationstyp:	Zeitschriftenaufsatz
Nutzungsrechte:	CC BY
Informationen zu den Nutzungsrechten:	https://creativecommons.org/licenses/by/4.0/
Zeitschrift:	EJNMMI Research 8
Seitenzahl oder Artikelnummer:	Art. 16
Verlag:	Springer
Verlagsort:	Berlin
Erscheinungsdatum:	2018
ISSN:	2191-219X
URL der Originalveröffentlichung:	http://dx.doi.org/10.1186/s13550-018-0372-x
DOI der Originalveröffentlichung:	10.1186/s13550-018-0372-x
Enthalten in den Sammlungen:	JGU-Publikationen