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Open AccessArticle

Recent Insights in Barium-131 as a Diagnostic Match for Radium-223: Cyclotron Production, Separation, Radiolabeling, and Imaging

1
Helmholtz-Zentrum Dresden-Rossendorf, Institut für Radiopharmazeutische Krebsforschung, Bautzner Landstraße 400, D-01328 Dresden, Germany
2
Fakultät Chemie und Lebensmittelchemie, Technische Universität Dresden, D-01062 Dresden, Germany
*
Author to whom correspondence should be addressed.
This article is dedicated to Prof. Dr. Ralf Miethchen (University of Rostock) on the occasion of his 80th birthday.
These authors contributed equally.
Pharmaceuticals 2020, 13(10), 272; https://doi.org/10.3390/ph13100272
Received: 31 August 2020 / Revised: 21 September 2020 / Accepted: 22 September 2020 / Published: 25 September 2020
(This article belongs to the Section Radiopharmaceutical Sciences)
Barium-131 is a single photon emission computed tomography (SPECT)-compatible radionuclide for nuclear medicine and a promising diagnostic match for radium-223/-224. Herein, we report on the sufficient production route 133Cs(p,3n)131Ba by using 27.5 MeV proton beams. An average of 190 MBq barium-131 per irradiation was obtained. The SR Resin-based purification process led to barium-131 in high radiochemical purity. An isotopic impurity of 0.01% barium-133 was detectable. For the first time, radiolabeling of the ligand macropa with barium-131 was performed. Radiolabeling methods under mild conditions and reaction controls based on TLC systems were successfully applied. Small animal SPECT/ computed tomography (CT) measurements and biodistribution studies were performed using [131Ba]Ba(NO3)2 as reference and 131Ba-labeled macropa in healthy mice for the first time. Biodistribution studies revealed the expected rapid bone uptake of [131Ba]Ba2+, whereas 131Ba-labeled macropa showed a fast clearance from the blood, thereby showing a significantly (p < 0.001) lower accumulation in the bone. We conclude that barium-131 is a promising SPECT radionuclide and delivers appropriate imaging qualities in small animals. Furthermore, the relative stability of the 131Ba-labeled macropa complex in vivo forms the basis for the development of sufficient new chelators, especially for radium isotopes. Thereby, barium-131 will attain its goal as a diagnostic match to the alpha emitters radium-223 and radium-224. View Full-Text
Keywords: barium-131; cyclotron production; radionuclide separation; macropa; small animal SPECT barium-131; cyclotron production; radionuclide separation; macropa; small animal SPECT
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MDPI and ACS Style

Reissig, F.; Bauer, D.; Ullrich, M.; Kreller, M.; Pietzsch, J.; Mamat, C.; Kopka, K.; Pietzsch, H.-J.; Walther, M. Recent Insights in Barium-131 as a Diagnostic Match for Radium-223: Cyclotron Production, Separation, Radiolabeling, and Imaging. Pharmaceuticals 2020, 13, 272.

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