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The label matters : µPET imaging of the biodistribution of low molar mass 89Zr and 18F-labeled poly(2-ethyl-2-oxazoline)

(2017) BIOMACROMOLECULES. 18(1). p.96-102
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Abstract
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-89 and F-18. F-18-labeled PEtOx is prepared by the strain-promoted azide-alkyne cycloaddition (SPAAC) of [F-18]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-89-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-18]-PEtOx displays a rapid and efficient clearance from the kidneys, 5 kDa [Zr-89]-Df-PEtOx is not efficiently cleared over the time course of the study, which is most likely caused by trapping of Zr-89-labeled metabolites in the renal tubules and not the polymer itself, demonstrating,the importance of selecting the appropriate label for biodistribution studies.
Keywords
POSITRON-EMISSION-TOMOGRAPHY, POLY(ETHYLENE GLYCOL), MOLECULAR-WEIGHT, DRUG-DELIVERY, POLY(2-OXAZOLINE)S, PROTEINS, ALTERNATIVES, CONJUGATION, COPOLYMERS, STRATEGIES

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Chicago
Glassner, Mathias, Luca Palmieri, Bryn Monnery, Thomas Verbrugghen, Steven Deleye, Sigrid Stroobants, Steven Staelens, Leonie Wyffels, and Richard Hoogenboom. 2017. “The Label Matters : µPET Imaging of the Biodistribution of Low Molar Mass 89Zr and 18F-labeled Poly(2-ethyl-2-oxazoline).” Biomacromolecules 18 (1): 96–102.
APA
Glassner, M., Palmieri, L., Monnery, B., Verbrugghen, T., Deleye, S., Stroobants, S., Staelens, S., et al. (2017). The label matters : µPET imaging of the biodistribution of low molar mass 89Zr and 18F-labeled poly(2-ethyl-2-oxazoline). BIOMACROMOLECULES, 18(1), 96–102.
Vancouver
1.
Glassner M, Palmieri L, Monnery B, Verbrugghen T, Deleye S, Stroobants S, et al. The label matters : µPET imaging of the biodistribution of low molar mass 89Zr and 18F-labeled poly(2-ethyl-2-oxazoline). BIOMACROMOLECULES. 2017;18(1):96–102.
MLA
Glassner, Mathias, Luca Palmieri, Bryn Monnery, et al. “The Label Matters : µPET Imaging of the Biodistribution of Low Molar Mass 89Zr and 18F-labeled Poly(2-ethyl-2-oxazoline).” BIOMACROMOLECULES 18.1 (2017): 96–102. Print.
@article{8516315,
  abstract     = {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-89 and F-18. F-18-labeled PEtOx is prepared by the strain-promoted azide-alkyne cycloaddition (SPAAC) of [F-18]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-89-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-18]-PEtOx displays a rapid and efficient clearance from the kidneys, 5 kDa [Zr-89]-Df-PEtOx is not efficiently cleared over the time course of the study, which is most likely caused by trapping of Zr-89-labeled metabolites in the renal tubules and not the polymer itself, demonstrating,the importance of selecting the appropriate label for biodistribution studies.},
  author       = {Glassner, Mathias and Palmieri, Luca and Monnery, Bryn and Verbrugghen, Thomas and Deleye, Steven and Stroobants, Sigrid and Staelens, Steven and Wyffels, Leonie and Hoogenboom, Richard},
  issn         = {1525-7797},
  journal      = {BIOMACROMOLECULES},
  keyword      = {POSITRON-EMISSION-TOMOGRAPHY,POLY(ETHYLENE GLYCOL),MOLECULAR-WEIGHT,DRUG-DELIVERY,POLY(2-OXAZOLINE)S,PROTEINS,ALTERNATIVES,CONJUGATION,COPOLYMERS,STRATEGIES},
  language     = {eng},
  number       = {1},
  pages        = {96--102},
  title        = {The label matters : {\textmu}PET imaging of the biodistribution of low molar mass 89Zr and 18F-labeled poly(2-ethyl-2-oxazoline)},
  url          = {http://dx.doi.org/10.1021/acs.biomac.6b01392},
  volume       = {18},
  year         = {2017},
}

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