Recent Insights in Barium-131 as a Diagnostic Match for Radium-223: Cyclotron Production, Separation, Radiolabeling, and Imaging
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 <sup>133</sup>Cs(<i>p</i>,<i>3n</i>)<sup&g...
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| Format: | Article |
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MDPI AG
2020-09-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/13/10/272 |
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| author | Falco Reissig David Bauer Martin Ullrich Martin Kreller Jens Pietzsch Constantin Mamat Klaus Kopka Hans-Jürgen Pietzsch Martin Walther |
| author_facet | Falco Reissig David Bauer Martin Ullrich Martin Kreller Jens Pietzsch Constantin Mamat Klaus Kopka Hans-Jürgen Pietzsch Martin Walther |
| author_sort | Falco Reissig |
| collection | DOAJ |
| description | 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 <sup>133</sup>Cs(<i>p</i>,<i>3n</i>)<sup>131</sup>Ba 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 [<sup>131</sup>Ba]Ba(NO<sub>3</sub>)<sub>2</sub> as reference and <sup>131</sup>Ba-labeled macropa in healthy mice for the first time. Biodistribution studies revealed the expected rapid bone uptake of [<sup>131</sup>Ba]Ba<sup>2+</sup>, whereas <sup>131</sup>Ba-labeled macropa showed a fast clearance from the blood, thereby showing a significantly (<i>p</i> < 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 <sup>131</sup>Ba-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. |
| first_indexed | 2024-03-10T16:03:08Z |
| format | Article |
| id | doaj.art-d47137eec1fc4101b331b6b8c56d1e9f |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T16:03:08Z |
| publishDate | 2020-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-d47137eec1fc4101b331b6b8c56d1e9f2023-11-20T15:07:49ZengMDPI AGPharmaceuticals1424-82472020-09-01131027210.3390/ph13100272Recent Insights in Barium-131 as a Diagnostic Match for Radium-223: Cyclotron Production, Separation, Radiolabeling, and ImagingFalco Reissig0David Bauer1Martin Ullrich2Martin Kreller3Jens Pietzsch4Constantin Mamat5Klaus Kopka6Hans-Jürgen Pietzsch7Martin Walther8Helmholtz-Zentrum Dresden-Rossendorf, Institut für Radiopharmazeutische Krebsforschung, Bautzner Landstraße 400, D-01328 Dresden, GermanyHelmholtz-Zentrum Dresden-Rossendorf, Institut für Radiopharmazeutische Krebsforschung, Bautzner Landstraße 400, D-01328 Dresden, GermanyHelmholtz-Zentrum Dresden-Rossendorf, Institut für Radiopharmazeutische Krebsforschung, Bautzner Landstraße 400, D-01328 Dresden, GermanyHelmholtz-Zentrum Dresden-Rossendorf, Institut für Radiopharmazeutische Krebsforschung, Bautzner Landstraße 400, D-01328 Dresden, GermanyHelmholtz-Zentrum Dresden-Rossendorf, Institut für Radiopharmazeutische Krebsforschung, Bautzner Landstraße 400, D-01328 Dresden, GermanyHelmholtz-Zentrum Dresden-Rossendorf, Institut für Radiopharmazeutische Krebsforschung, Bautzner Landstraße 400, D-01328 Dresden, GermanyHelmholtz-Zentrum Dresden-Rossendorf, Institut für Radiopharmazeutische Krebsforschung, Bautzner Landstraße 400, D-01328 Dresden, GermanyHelmholtz-Zentrum Dresden-Rossendorf, Institut für Radiopharmazeutische Krebsforschung, Bautzner Landstraße 400, D-01328 Dresden, GermanyHelmholtz-Zentrum Dresden-Rossendorf, Institut für Radiopharmazeutische Krebsforschung, Bautzner Landstraße 400, D-01328 Dresden, GermanyBarium-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 <sup>133</sup>Cs(<i>p</i>,<i>3n</i>)<sup>131</sup>Ba 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 [<sup>131</sup>Ba]Ba(NO<sub>3</sub>)<sub>2</sub> as reference and <sup>131</sup>Ba-labeled macropa in healthy mice for the first time. Biodistribution studies revealed the expected rapid bone uptake of [<sup>131</sup>Ba]Ba<sup>2+</sup>, whereas <sup>131</sup>Ba-labeled macropa showed a fast clearance from the blood, thereby showing a significantly (<i>p</i> < 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 <sup>131</sup>Ba-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.https://www.mdpi.com/1424-8247/13/10/272barium-131cyclotron productionradionuclide separationmacropasmall animal SPECT |
| spellingShingle | Falco Reissig David Bauer Martin Ullrich Martin Kreller Jens Pietzsch Constantin Mamat Klaus Kopka Hans-Jürgen Pietzsch Martin Walther Recent Insights in Barium-131 as a Diagnostic Match for Radium-223: Cyclotron Production, Separation, Radiolabeling, and Imaging Pharmaceuticals barium-131 cyclotron production radionuclide separation macropa small animal SPECT |
| title | Recent Insights in Barium-131 as a Diagnostic Match for Radium-223: Cyclotron Production, Separation, Radiolabeling, and Imaging |
| title_full | Recent Insights in Barium-131 as a Diagnostic Match for Radium-223: Cyclotron Production, Separation, Radiolabeling, and Imaging |
| title_fullStr | Recent Insights in Barium-131 as a Diagnostic Match for Radium-223: Cyclotron Production, Separation, Radiolabeling, and Imaging |
| title_full_unstemmed | Recent Insights in Barium-131 as a Diagnostic Match for Radium-223: Cyclotron Production, Separation, Radiolabeling, and Imaging |
| title_short | Recent Insights in Barium-131 as a Diagnostic Match for Radium-223: Cyclotron Production, Separation, Radiolabeling, and Imaging |
| title_sort | recent insights in barium 131 as a diagnostic match for radium 223 cyclotron production separation radiolabeling and imaging |
| topic | barium-131 cyclotron production radionuclide separation macropa small animal SPECT |
| url | https://www.mdpi.com/1424-8247/13/10/272 |
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