Sub‐10 nm Radiolabeled Barium Sulfate Nanoparticles as Carriers for Theranostic Applications and Targeted Alpha Therapy

Abstract The treatment of cancer patients with α‐particle‐emitting therapeutics continues to gain in importance and relevance. The range of radiopharmaceutically relevant α‐emitters is limited to a few radionuclides, as stable chelators or carrier systems for safe transport of the radioactive cargo...

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Main Authors: Falco Reissig, Dr. Kristof Zarschler, Dr. René Hübner, Dr. Hans‐Jürgen Pietzsch, Prof. Dr. Klaus Kopka, Dr. Constantin Mamat
Format: Article
Language:English
Published: Wiley-VCH 2020-08-01
Series:ChemistryOpen
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Online Access:https://doi.org/10.1002/open.202000126
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author Falco Reissig
Dr. Kristof Zarschler
Dr. René Hübner
Dr. Hans‐Jürgen Pietzsch
Prof. Dr. Klaus Kopka
Dr. Constantin Mamat
author_facet Falco Reissig
Dr. Kristof Zarschler
Dr. René Hübner
Dr. Hans‐Jürgen Pietzsch
Prof. Dr. Klaus Kopka
Dr. Constantin Mamat
author_sort Falco Reissig
collection DOAJ
description Abstract The treatment of cancer patients with α‐particle‐emitting therapeutics continues to gain in importance and relevance. The range of radiopharmaceutically relevant α‐emitters is limited to a few radionuclides, as stable chelators or carrier systems for safe transport of the radioactive cargo are often lacking. Encapsulation of α‐emitters into solid inorganic systems can help to diversify the portfolio of candidate radionuclides, provided, that these nanomaterials effectively retain both the parent and the recoil daughters. We therefore focus on designing stable and defined nanocarrier‐based systems for various clinically relevant radionuclides, including the promising α‐emitting radionuclide 224Ra. Hence, sub‐10 nm barium sulfate nanocontainers were prepared and different radiometals like 89Zr, 111In, 131Ba, 177Lu or 224Ra were incorporated. Our system shows stabilities of >90 % regarding the radiometal release from the BaSO4 matrix. Furthermore, we confirm the presence of surface‐exposed amine functionalities as well as the formation of a biomolecular corona.
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spelling doaj.art-438f32c0cb654ab9b3871122b6845a962022-12-21T22:44:49ZengWiley-VCHChemistryOpen2191-13632020-08-019879780510.1002/open.202000126Sub‐10 nm Radiolabeled Barium Sulfate Nanoparticles as Carriers for Theranostic Applications and Targeted Alpha TherapyFalco Reissig0Dr. Kristof Zarschler1Dr. René Hübner2Dr. Hans‐Jürgen Pietzsch3Prof. Dr. Klaus Kopka4Dr. Constantin Mamat5Institute of Radiopharmaceutical Cancer Research Helmholtz-Zentrum Dresden-Rossendorf Bautzner Landstraße 400 01328 Dresden GermanyInstitute of Radiopharmaceutical Cancer Research Helmholtz-Zentrum Dresden-Rossendorf Bautzner Landstraße 400 01328 Dresden GermanyInstitute of Ion Beam Physics and Materials Research Helmholtz-Zentrum Dresden-Rossendorf Bautzner Landstraße 400 01328 Dresden GermanyInstitute of Radiopharmaceutical Cancer Research Helmholtz-Zentrum Dresden-Rossendorf Bautzner Landstraße 400 01328 Dresden GermanyInstitute of Radiopharmaceutical Cancer Research Helmholtz-Zentrum Dresden-Rossendorf Bautzner Landstraße 400 01328 Dresden GermanyInstitute of Radiopharmaceutical Cancer Research Helmholtz-Zentrum Dresden-Rossendorf Bautzner Landstraße 400 01328 Dresden GermanyAbstract The treatment of cancer patients with α‐particle‐emitting therapeutics continues to gain in importance and relevance. The range of radiopharmaceutically relevant α‐emitters is limited to a few radionuclides, as stable chelators or carrier systems for safe transport of the radioactive cargo are often lacking. Encapsulation of α‐emitters into solid inorganic systems can help to diversify the portfolio of candidate radionuclides, provided, that these nanomaterials effectively retain both the parent and the recoil daughters. We therefore focus on designing stable and defined nanocarrier‐based systems for various clinically relevant radionuclides, including the promising α‐emitting radionuclide 224Ra. Hence, sub‐10 nm barium sulfate nanocontainers were prepared and different radiometals like 89Zr, 111In, 131Ba, 177Lu or 224Ra were incorporated. Our system shows stabilities of >90 % regarding the radiometal release from the BaSO4 matrix. Furthermore, we confirm the presence of surface‐exposed amine functionalities as well as the formation of a biomolecular corona.https://doi.org/10.1002/open.202000126radiolabelingradiumnanoencapsulationradiooncologybariumtherapeutic applications
spellingShingle Falco Reissig
Dr. Kristof Zarschler
Dr. René Hübner
Dr. Hans‐Jürgen Pietzsch
Prof. Dr. Klaus Kopka
Dr. Constantin Mamat
Sub‐10 nm Radiolabeled Barium Sulfate Nanoparticles as Carriers for Theranostic Applications and Targeted Alpha Therapy
ChemistryOpen
radiolabeling
radium
nanoencapsulation
radiooncology
barium
therapeutic applications
title Sub‐10 nm Radiolabeled Barium Sulfate Nanoparticles as Carriers for Theranostic Applications and Targeted Alpha Therapy
title_full Sub‐10 nm Radiolabeled Barium Sulfate Nanoparticles as Carriers for Theranostic Applications and Targeted Alpha Therapy
title_fullStr Sub‐10 nm Radiolabeled Barium Sulfate Nanoparticles as Carriers for Theranostic Applications and Targeted Alpha Therapy
title_full_unstemmed Sub‐10 nm Radiolabeled Barium Sulfate Nanoparticles as Carriers for Theranostic Applications and Targeted Alpha Therapy
title_short Sub‐10 nm Radiolabeled Barium Sulfate Nanoparticles as Carriers for Theranostic Applications and Targeted Alpha Therapy
title_sort sub 10 nm radiolabeled barium sulfate nanoparticles as carriers for theranostic applications and targeted alpha therapy
topic radiolabeling
radium
nanoencapsulation
radiooncology
barium
therapeutic applications
url https://doi.org/10.1002/open.202000126
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