Astatine-211-Labeled Gold Nanoparticles for Targeted Alpha-Particle Therapy via Intravenous Injection
Alpha-particle radiotherapy has gained considerable attention owing to its potent anti-cancer effect. <sup>211</sup>At, with a relatively short half-life of 7.2 h, emits an alpha particle within a few cell diameters with high kinetic energy, which damages cancer cells with high biologica...
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MDPI AG
2022-12-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/12/2705 |
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| author | Xuhao Huang Kazuko Kaneda-Nakashima Yuichiro Kadonaga Kazuya Kabayama Atsushi Shimoyama Kazuhiro Ooe Hiroki Kato Atsushi Toyoshima Atsushi Shinohara Hiromitsu Haba Yang Wang Koichi Fukase |
| author_facet | Xuhao Huang Kazuko Kaneda-Nakashima Yuichiro Kadonaga Kazuya Kabayama Atsushi Shimoyama Kazuhiro Ooe Hiroki Kato Atsushi Toyoshima Atsushi Shinohara Hiromitsu Haba Yang Wang Koichi Fukase |
| author_sort | Xuhao Huang |
| collection | DOAJ |
| description | Alpha-particle radiotherapy has gained considerable attention owing to its potent anti-cancer effect. <sup>211</sup>At, with a relatively short half-life of 7.2 h, emits an alpha particle within a few cell diameters with high kinetic energy, which damages cancer cells with high biological effectiveness. In this study, we investigated the intravenous injection of <sup>211</sup>At-labeled gold nanoparticles (AuNPs) for targeted alpha-particle therapy (TAT). Different kinds of surface-modified gold nanoparticles can be labeled with <sup>211</sup>At in high radiochemical yield in 5 min, and no purification is necessary. The in vivo biodistribution results showed the accumulation of 5 nm <sup>211</sup>At-AuNPs@mPEG at 2.25% injection dose per gram (% ID/g) in tumors within 3 h via the enhanced permeability and retention (EPR) effect. Additionally, we observed a long retention time in tumor tissues within 24 h. This is the first study to demonstrate the anti-tumor efficacy of 5 nm <sup>211</sup>At-AuNPs@mPEG that can significantly suppress tumor growth in a pancreatic cancer model via intravenous administration. AuNPs are satisfactory carriers for <sup>211</sup>At delivery, due to simple and efficient synthesis processes and high stability. The intravenous administration of 5 nm <sup>211</sup>At-AuNPs@mPEG has a significant anti-tumor effect. This study provides a new framework for designing nanoparticles suitable for targeted alpha-particle therapy via intravenous injection. |
| first_indexed | 2024-03-09T15:58:32Z |
| format | Article |
| id | doaj.art-94ddafdf4dda4674aa72f1ad12a409e9 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T15:58:32Z |
| publishDate | 2022-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-94ddafdf4dda4674aa72f1ad12a409e92023-11-24T17:20:36ZengMDPI AGPharmaceutics1999-49232022-12-011412270510.3390/pharmaceutics14122705Astatine-211-Labeled Gold Nanoparticles for Targeted Alpha-Particle Therapy via Intravenous InjectionXuhao Huang0Kazuko Kaneda-Nakashima1Yuichiro Kadonaga2Kazuya Kabayama3Atsushi Shimoyama4Kazuhiro Ooe5Hiroki Kato6Atsushi Toyoshima7Atsushi Shinohara8Hiromitsu Haba9Yang Wang10Koichi Fukase11Department of Chemistry, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, JapanDivision of Science, Institute for Radiation Sciences, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, JapanDepartment of Nuclear Medicine and Tracer Kinetics, Osaka University Graduate School of Medicine, 2-2 Yamadaoka, Suita 565-0871, Osaka, JapanDepartment of Chemistry, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, JapanDepartment of Chemistry, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, JapanDivision of Science, Institute for Radiation Sciences, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, JapanDepartment of Nuclear Medicine and Tracer Kinetics, Osaka University Graduate School of Medicine, 2-2 Yamadaoka, Suita 565-0871, Osaka, JapanDivision of Science, Institute for Radiation Sciences, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, JapanDivision of Science, Institute for Radiation Sciences, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, JapanNishina Center for Accelerator-Based Science, RIKEN, 2-1 Hirosawa, Wako 351-0198, Saitama, JapanNishina Center for Accelerator-Based Science, RIKEN, 2-1 Hirosawa, Wako 351-0198, Saitama, JapanDepartment of Chemistry, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, JapanAlpha-particle radiotherapy has gained considerable attention owing to its potent anti-cancer effect. <sup>211</sup>At, with a relatively short half-life of 7.2 h, emits an alpha particle within a few cell diameters with high kinetic energy, which damages cancer cells with high biological effectiveness. In this study, we investigated the intravenous injection of <sup>211</sup>At-labeled gold nanoparticles (AuNPs) for targeted alpha-particle therapy (TAT). Different kinds of surface-modified gold nanoparticles can be labeled with <sup>211</sup>At in high radiochemical yield in 5 min, and no purification is necessary. The in vivo biodistribution results showed the accumulation of 5 nm <sup>211</sup>At-AuNPs@mPEG at 2.25% injection dose per gram (% ID/g) in tumors within 3 h via the enhanced permeability and retention (EPR) effect. Additionally, we observed a long retention time in tumor tissues within 24 h. This is the first study to demonstrate the anti-tumor efficacy of 5 nm <sup>211</sup>At-AuNPs@mPEG that can significantly suppress tumor growth in a pancreatic cancer model via intravenous administration. AuNPs are satisfactory carriers for <sup>211</sup>At delivery, due to simple and efficient synthesis processes and high stability. The intravenous administration of 5 nm <sup>211</sup>At-AuNPs@mPEG has a significant anti-tumor effect. This study provides a new framework for designing nanoparticles suitable for targeted alpha-particle therapy via intravenous injection.https://www.mdpi.com/1999-4923/14/12/2705astatine-211gold nanoparticlestargeted alpha-particle therapycancer therapypancreatic cancerintravenous administration |
| spellingShingle | Xuhao Huang Kazuko Kaneda-Nakashima Yuichiro Kadonaga Kazuya Kabayama Atsushi Shimoyama Kazuhiro Ooe Hiroki Kato Atsushi Toyoshima Atsushi Shinohara Hiromitsu Haba Yang Wang Koichi Fukase Astatine-211-Labeled Gold Nanoparticles for Targeted Alpha-Particle Therapy via Intravenous Injection Pharmaceutics astatine-211 gold nanoparticles targeted alpha-particle therapy cancer therapy pancreatic cancer intravenous administration |
| title | Astatine-211-Labeled Gold Nanoparticles for Targeted Alpha-Particle Therapy via Intravenous Injection |
| title_full | Astatine-211-Labeled Gold Nanoparticles for Targeted Alpha-Particle Therapy via Intravenous Injection |
| title_fullStr | Astatine-211-Labeled Gold Nanoparticles for Targeted Alpha-Particle Therapy via Intravenous Injection |
| title_full_unstemmed | Astatine-211-Labeled Gold Nanoparticles for Targeted Alpha-Particle Therapy via Intravenous Injection |
| title_short | Astatine-211-Labeled Gold Nanoparticles for Targeted Alpha-Particle Therapy via Intravenous Injection |
| title_sort | astatine 211 labeled gold nanoparticles for targeted alpha particle therapy via intravenous injection |
| topic | astatine-211 gold nanoparticles targeted alpha-particle therapy cancer therapy pancreatic cancer intravenous administration |
| url | https://www.mdpi.com/1999-4923/14/12/2705 |
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