The Label Matters: μPET Imaging of the Biodistribution of Low Molar Mass 89 Zr and 18 F-Labeled Poly(2-ethyl-2-oxazoline)

Poly(2-alkyl-2-oxazoline)s (PAOx) have received increasing interest for biomedical applications. Therefore, it is of fundamental importance to gain an in-depth understanding of the biodistribution profile of PAOx. We report the biodistribution of poly(2-ethyl-2-oxazoline) (PEtOx) with a molar mass o...

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Bibliographic Details
Published in:Biomacromolecules 2017-01, Vol.18 (1), p.96-102
Main Authors: Glassner, Mathias, Palmieri, Luca, Monnery, Bryn D, Verbrugghen, Thomas, Deleye, Steven, Stroobants, Sigrid, Staelens, Steven, Wyffels, Leonie, Hoogenboom, Richard
Format: Article
Language:English
Subjects:
Animals
Fluorine Radioisotopes - chemistry
Fluorine Radioisotopes - pharmacokinetics
Image Processing, Computer-Assisted
Liver - diagnostic imaging
Liver - metabolism
Metabolic Clearance Rate
Mice
Mice, Inbred C57BL
Polyamines - chemistry
Polymers - chemistry
Polymers - pharmacokinetics
Positron-Emission Tomography - methods
Radiopharmaceuticals - chemistry
Radiopharmaceuticals - pharmacokinetics
Tissue Distribution
Zirconium - chemistry
Zirconium - pharmacokinetics
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Summary:Poly(2-alkyl-2-oxazoline)s (PAOx) have received increasing interest for biomedical applications. Therefore, it is of fundamental importance to gain an in-depth understanding of the biodistribution profile of PAOx. We report the biodistribution of poly(2-ethyl-2-oxazoline) (PEtOx) with a molar mass of 5 kDa radiolabeled with PET isotopes Zr and F. F-labeled PEtOx is prepared by the strain-promoted azide-alkyne cycloaddition (SPAAC) of [ F]fluoroethylazide to bicyclo[6.1.0]non-4-yne (BCN)-functionalized PEtOx as many common labeling strategies were found to be unsuccessful for PEtOx. Zr-labeled PEtOx is prepared using desferrioxamine end-groups as a chelator. Five kDa PEtOx shows a significantly faster blood clearance compared to PEtOx of higher molar mass while uptake in the liver is lower, indicating a minor contribution of the liver in excretion of the 5 kDa PEtOx. While [ F]-PEtOx displays a rapid and efficient clearance from the kidneys, 5 kDa [ Zr]-Df-PEtOx is not efficiently cleared over the time course of the study, which is most likely caused by trapping of Zr-labeled metabolites in the renal tubules and not the polymer itself, demonstrating the importance of selecting the appropriate label for biodistribution studies.
ISSN:1525-7797
1526-4602
DOI:10.1021/acs.biomac.6b01392