Nano-hydroxyapatite radiolabeled with radium dichloride [223Ra] RaCl2 for bone cancer targeted alpha therapy: In vitro assay and radiation effect on the nanostructure

Sara Gemini-Piperni; Eduardo Ricci-Junior; Derya İlem-Özdemir; Beatriz da Silva Batista; Luciana Magalhães Rebelo Alencar; Alexandre Malta Rossi; Ralph Santos-Oliveira

doi:10.1016/j.colsurfb.2023.113174

Nano-hydroxyapatite radiolabeled with radium dichloride [²²³Ra] RaCl₂ for bone cancer targeted alpha therapy: In vitro assay and radiation effect on the nanostructure

Colloids Surf B Biointerfaces. 2023 Mar:223:113174. doi: 10.1016/j.colsurfb.2023.113174. Epub 2023 Jan 26.

Authors

Sara Gemini-Piperni¹, Eduardo Ricci-Junior², Derya İlem-Özdemir³, Beatriz da Silva Batista⁴, Luciana Magalhães Rebelo Alencar⁵, Alexandre Malta Rossi⁶, Ralph Santos-Oliveira⁷

Affiliations

¹ Laboratory of Bioengineering and Nanostructure Biomaterials, Institute of Biomedical Science, Federal Univsersity of Rio de Janeiro, 21941906, Brazil.
² Laboratory of Nanomedicine, College of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro 21941902, Brazil.
³ Ege University, Faculty of Pharmacy, Department of Radiopharmacy, Bornova, Izmir 35040, Turkey.
⁴ Center for Social Sciences, Health and Technology, Federal University of Maranhão, Maranhão 65915-240, Brazil.
⁵ Center for Social Sciences, Health and Technology, Federal University of Maranhão, Maranhão 65915-240, Brazil; Department of Physics, Laboratory of Biophysics and Nanosystems, Federal University of Maranhão, Maranhão 65080-805, Brazil.
⁶ Department of Condensed Matter, Applied Physics and Nanoscience, Brazilian Center for Research in Physics, Rio de Janeiro 22290-180, Brazil.
⁷ Brazilian Nuclear Energy Commission, Nuclear Engineering Institute, Laboratory of Nanoradiopharmaceuticals and Synthesis of Novel Radiopharmaceuticals, Rio de Janeiro 21941906, Brazil; Rio de Janeiro State University, Laboratory of Radiopharmacy and Nanoradiopharmaceuticals, Rio de Janeiro 2320000, Brazil. Electronic address: roliveira@ien.gov.br.

PMID: 36746067
DOI: 10.1016/j.colsurfb.2023.113174

Abstract

The use of targeted alpha therapy (TAT) for bone cancer is increasing each year. Among the alpha radionuclides, radium [²²³Ra]Ra⁺² is the first one approved for bone cancer metastasis therapy. The development of novel radiopharmaceutical based on [²²³Ra]Ra⁺² is essential to continuously increase the arsenal of new TAT drugs. In this study we have developed, characterized, and in vitro evaluated [²²³Ra] Ra-nano-hydroxyapatite. The results showed that [²²³Ra] Ra-nano-hydroxyapatite has a dose-response relationship for osteosarcoma cells and a safety profile for human fibroblast cells, corroborating the application as a radiopharmaceutical.

Keywords: Osteosarcoma; Radiopharmaceutical; Targeted alpha therapy.

MeSH terms

Bone Neoplasms* / drug therapy
Humans
Nanostructures*
Osteosarcoma* / drug therapy
Radiopharmaceuticals
Radium* / chemistry
Radium* / therapeutic use

Substances

Radiopharmaceuticals
Radium