Preparation of Zirconium-89 Solutions for Radiopharmaceutical Purposes: Interrelation Between Formulation, Radiochemical Purity, Stability and Biodistribution.

Author(s) Larenkov, A.; Bubenschikov, V.; Makichyan, A.; Zhukova, M.; Krasnoperova, A.; Kodina, G.
Journal Molecules
Date Published 2019 Apr 18
Abstract

Zirconium-89 is a promising radionuclide for nuclear medicine. The aim of the present work was to find a suitable method for obtaining zirconium-89 solutions for radiopharmaceutical purposes. For this purpose, the ion exchange behavior of zirconium-89 solutions was studied. Radio-TLC (thin layer chromatography) and biodistribution studies were carried out to understand speciation of zirconium-89 complexes and their role in the development of new radiopharmaceuticals. Three methods of zirconium-89 isolation were studied using ZR (hydroxamate) and Chelex-100 resins. It was found that ZR-resin alone is not enough to obtain stable zirconium-89 formulations. An easy and effective method of reconstitution of [Zr]Zr-oxalate to [Zr]Zr-citrate using Chelex-100 resin was developed. Developed procedures allow obtaining [Zr]Zr-oxalate (in 0.1 M sodium oxalate solution) and [Zr]Zr-citrate (in 0.1-1.0 M sodium citrate solution). These solutions are perfectly suitable and convenient for radiopharmaceutical purposes. Our results prove [Zr]Zr-citrate to be advantageous over [Zr]Zr-oxalate. During evaluation of speciation of zirconium-89 complexes, a new TLC method was developed, since it was proved that there is no comprehensive method for analysis or zirconium-89 preparations. The new method provides valuable insights about the content of "active" ionic form of zirconium-89. The interrelation of the chromatographic behavior of zirconium-89 preparations and their biodistribution was studied.

DOI 10.3390/molecules24081534
ISSN 1420-3049
Citation Larenkov A, Bubenschikov V, Makichyan A, Zhukova M, Krasnoperova A, Kodina G. Preparation of Zirconium-89 Solutions for Radiopharmaceutical Purposes: Interrelation Between Formulation, Radiochemical Purity, Stability and Biodistribution. Molecules. 2019;24(8).