Targeted Radium Alpha Therapy in the Era of Nanomedicine: In Vivo Results

• Published in: International journal of molecular sciences Vol. 25; no. 1; p. 664
• Main Authors: Trencsényi, György, Csikos, Csaba, Képes, Zita
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 01-01-2024; MDPI
• Subjects: Acids; Cancer therapies; Clinical trials; Cytotoxicity; Drug dosages; Ethylenediaminetetraacetic acid; Health aspects; Metastasis; Nanoparticles; Peptides; preclinical; Quantum dots; Radiation; Radiation therapy; Radioisotopes; Radiotherapy; Radium-223/224 (223/224Ra); Review; targeted alpha-particle therapy; Tumors; xenotransplants; nanoparticles; preclinical; Radium-223/224 (223/224Ra); targeted alpha-particle therapy; xenotransplants
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms25010664

Targeted alpha-particle therapy using radionuclides with alpha emission is a rapidly developing area in modern cancer treatment. To selectively deliver alpha-emitting isotopes to tumors, targeting vectors, including monoclonal antibodies, peptides, small molecule inhibitors, or other biomolecules, are attached to them, which ensures specific binding to tumor-related antigens and cell surface receptors. Although earlier studies have already demonstrated the anti-tumor potential of alpha-emitting radium (Ra) isotopes-Radium-223 and Radium-224 (
Ra)-in the treatment of skeletal metastases, their inability to complex with target-specific moieties hindered application beyond bone targeting. To exploit the therapeutic gains of Ra across a wider spectrum of cancers, nanoparticles have recently been embraced as carriers to ensure the linkage of
Ra to target-affine vectors. Exemplified by prior findings, Ra was successfully bound to several nano/microparticles, including lanthanum phosphate, nanozeolites, barium sulfate, hydroxyapatite, calcium carbonate, gypsum, celestine, or liposomes. Despite the lengthened tumor retention and the related improvement in the radiotherapeutic effect of
Ra coupled to nanoparticles, the in vivo assessment of the radiolabeled nanoprobes is a prerequisite prior to clinical usage. For this purpose, experimental xenotransplant models of different cancers provide a well-suited scenario. Herein, we summarize the latest achievements with
Ra-doped nanoparticles and related advances in targeted alpha radiotherapy.