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Open AccessArticle

A Proof-of-Concept Study on the Therapeutic Potential of Au Nanoparticles Radiolabeled with the Alpha-Emitter Actinium-225

1
Institute of Nuclear & Radiological Sciences & Technology, Energy & Safety, National Center for Scientific Research “Demokritos”, 15341 Athens, Greece
2
Institute of Chemical Biology, National Hellenic Research Foundation, 11635 Athens, Greece
3
Institute of Biosciences and Applications, National Center for Scientific Research “Demokritos”, 15341 Athens, Greece
4
A’ Pathology Department, 401 General Military Hospital of Athens, 11525 Athens, Greece
5
ICMUB, UMR 6302 CNRS-UB, Université Bourgogne Franche-Comté, 21000 Dijon, France
6
Institut UTINAM, UMR 6213 CNRS-UBFC, Université Bourgogne Franche-Comté, 25030 Besançon, France
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(2), 188; https://doi.org/10.3390/pharmaceutics12020188
Received: 1 December 2019 / Revised: 20 January 2020 / Accepted: 19 February 2020 / Published: 21 February 2020
(This article belongs to the Special Issue Targeted Radionuclide Tumor Therapy)
Actinium-225 (225Ac) is receiving increased attention for its application in targeted radionuclide therapy, due to the short range of its emitted alpha particles in conjunction with their high linear energy transfer, which lead to the eradication of tumor cells while sparing neighboring healthy tissue. The objective of our study was the evaluation of a gold nanoparticle radiolabeled with 225Ac as an injectable radiopharmaceutical form of brachytherapy for local radiation treatment of cancer. [email protected] was radiolabeled with 225Ac at pH 5.6 (30 min at 70 °C), and in vitro stability was evaluated. In vitro cytotoxicity was assessed in U-87 MG cancer cells, and in vivo biodistribution was performed by intravenous and intratumoral administration of [225Ac]225[email protected] in U-87 MG tumor-bearing mice. A preliminary study to assess therapeutic efficacy of the intratumorally-injected radio-nanomedicine was performed over a period of 22 days, while the necrotic effect on tumors was evaluated by a histopathology study. We have shown that [225Ac]225[email protected] resulted in the retardation of tumor growth after its intratumoral injection in U87MG tumor-bearing mice, even though very low activities were injected per mouse. This gold nanoparticle radiopharmaceutical could be applied as an unconventional brachytherapy in injectable form for local radiation treatment of cancer. View Full-Text
Keywords: actinium-225; alpha emitters; gold nanoparticles; radiolabeling; brachytherapy; cancer therapy actinium-225; alpha emitters; gold nanoparticles; radiolabeling; brachytherapy; cancer therapy
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Salvanou, E.-A.; Stellas, D.; Tsoukalas, C.; Mavroidi, B.; Paravatou-Petsotas, M.; Kalogeropoulos, N.; Xanthopoulos, S.; Denat, F.; Laurent, G.; Bazzi, R.; Roux, S.; Bouziotis, P. A Proof-of-Concept Study on the Therapeutic Potential of Au Nanoparticles Radiolabeled with the Alpha-Emitter Actinium-225. Pharmaceutics 2020, 12, 188.

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