A<sup>224</sup>Ra-labeled polyoxopalladate as a putative radiopharmaceutical

Gott, Matthew; Yang, Peng; Kortz, Ulrich; Stephan, Holger; Pietzsch, Hans‐Jürgen; Mamat, Constantin

doi:10.1039/c9cc02587a

Cited by 32 publications

(28 citation statements)

References 29 publications

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“…Recently, the satisfactory immobilization of 223 Ra in NaA nanozeolites [140], magnetite nanoparticles [141], polyoxopalladate [142], hydroxyapatites [143] and CaCO 3 microparticles [144] has been developed.…”

Section: α-Emitting Radionuclidesmentioning

confidence: 99%

Targeted Radionuclide Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives

et al. 2020

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Prostate cancer is the most commonly diagnosed malignancy in men and the second leading cause of cancer-related deaths in Western civilization. Although localized prostate cancer can be treated effectively in different ways, almost all patients progress to the incurable metastatic castration-resistant prostate cancer. Due to the significant mortality and morbidity rate associated with the progression of this disease, there is an urgent need for new and targeted treatments. In this review, we summarize the recent advances in research on identification of prostate tissue-specific antigens for targeted therapy, generation of highly specific and selective molecules targeting these antigens, availability of therapeutic radionuclides for widespread medical applications, and recent achievements in the development of new-generation small-molecule inhibitors and antibody-based strategies for targeted prostate cancer therapy with alpha-, beta-, and Auger electron-emitting radionuclides.

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Section: α-Emitting Radionuclidesmentioning

confidence: 99%

Targeted Radionuclide Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives

et al. 2020

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“…Based on the determined extraction constants, calix[4]-tetraacetic seemed to be the most promising of the compounds studied. Recently, Mamat et al [ 12 ] evaluated polyoxopalladates for incorporation of radium radionuclides in the center of the complex. In 2020, a short report was published on the possibility of application a macrocycle ligand having a large complexation ring (MACROPA) for 223 Ra complexation [ 13 ].…”

Section: Introductionmentioning

confidence: 99%

Trastuzumab Modified Barium Ferrite Magnetic Nanoparticles Labeled with Radium-223: A New Potential Radiobioconjugate for Alpha Radioimmunotherapy

et al. 2020

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Barium ferrite nanoparticles (BaFeNPs) were investigated as vehicles for 223Ra radionuclide in targeted α-therapy. BaFe nanoparticles were labeled using a hydrothermal Ba2+ cations replacement by 223Ra with yield reaching 61.3 ± 1.8%. Radiolabeled nanoparticles were functionalized with 3-phosphonopropionic acid (CEPA) linker followed by covalent conjugation to trastuzumab (Herceptin®). Thermogravimetric analysis and radiometric method with the use of [131I]-labeled trastuzumab revealed that on average 19–21 molecules of trastuzumab are attached to the surface of one BaFe–CEPA nanoparticle. The hydrodynamic diameter of BaFe–CEPA–trastuzumab conjugate is 99.9 ± 3.0 nm in water and increases to 218.3 ± 3.7 nm in PBS buffer, and the zeta potential varies from +27.2 ± 0.7 mV in water to −8.8 ± 0.7 in PBS buffer. The [223Ra]BaFe–CEPA–trastuzumab radiobioconjugate almost quantitatively retained 223Ra (>98%) and about 96% of 211Bi and 94% of 211Pb over 30 days. The obtained radiobioconjugate exhibited high affinity, cell internalization and cytotoxicity towards the human ovarian adenocarcinoma SKOV-3 cells overexpressing HER2 receptor. Confocal studies indicated that [223Ra]BaFe–CEPA–trastuzumab was located in peri-nuclear space. High cytotoxicity of the [223Ra]BaFe–CEPA–trastuzumab bioconjugate was confirmed by radiotoxicity studies on SKOV-3 cell monolayers and 3D-spheroids. In addition, the magnetic properties of the radiobioconjugate should allow for its use in guide drug delivery driven by magnetic field gradient.

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“…As an alternative strategy to organic ligands, we and several other groups made substantial efforts to incorporate radium into nanocarrier-based systems, including polyoxopalladates, [17] hydroxyapatite, [18] iron oxide, [19] barium ferrite, or nanozeolites. [20] Recently, we reported on the development of a straightforward carrier system for radium based on barium sulfate nanoparticles (NPs).…”

Section: Introductionmentioning

confidence: 99%

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

et al. 2020

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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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A²²⁴Ra-labeled polyoxopalladate as a putative radiopharmaceutical

Abstract: A facile preparation of polyoxopalladates with enhanced properties containing radium-224 in the core and a protein corona for further functionalization with targeting (bio)molecules for therapeutic applications in oncology is described.

Cited by 32 publications

References 29 publications

Targeted Radionuclide Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives

Targeted Radionuclide Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives

Trastuzumab Modified Barium Ferrite Magnetic Nanoparticles Labeled with Radium-223: A New Potential Radiobioconjugate for Alpha Radioimmunotherapy

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

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A224Ra-labeled polyoxopalladate as a putative radiopharmaceutical

Abstract: A facile preparation of polyoxopalladates with enhanced properties containing radium-224 in the core and a protein corona for further functionalization with targeting (bio)molecules for therapeutic applications in oncology is described.

Cited by 32 publications

References 29 publications

Targeted Radionuclide Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives

Targeted Radionuclide Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives

Trastuzumab Modified Barium Ferrite Magnetic Nanoparticles Labeled with Radium-223: A New Potential Radiobioconjugate for Alpha Radioimmunotherapy

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

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A²²⁴Ra-labeled polyoxopalladate as a putative radiopharmaceutical