Iodinated Copper–Cysteamine Nanoparticles as Radiosensitizers for Tumor Radiotherapy

<b>Background/Objectives:</b> Radiotherapy is a widely applied first-line clinical treatment modality of cancer. Copper–cysteamine (Cu-Cy) nanoparticles represent a new type of photosensitizer that demonstrates significant anti-tumor potential by X-ray-induced photodynamic therapy. Iodid...

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Main Authors: Miaomiao Zhang, Yu Yang, Ying Xu, Jie Wang, Shihong Li
Format: Article
Language:English
Published: MDPI AG 2025-01-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/17/2/149
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author Miaomiao Zhang
Yu Yang
Ying Xu
Jie Wang
Shihong Li
author_facet Miaomiao Zhang
Yu Yang
Ying Xu
Jie Wang
Shihong Li
author_sort Miaomiao Zhang
collection DOAJ
description <b>Background/Objectives:</b> Radiotherapy is a widely applied first-line clinical treatment modality of cancer. Copper–cysteamine (Cu-Cy) nanoparticles represent a new type of photosensitizer that demonstrates significant anti-tumor potential by X-ray-induced photodynamic therapy. Iodide is a high-Z element with superior X-ray absorption ability and has the β-decay radiotherapeutic nuclide, <sup>131</sup>I, which emits Cherenkov light. In this study we aimed to investigate the X-ray-induced photodynamic therapy potential of iodinated Cu-Cy (Cu-Cy-I) nanoparticles and also explore the local treatment efficacy of <sup>131</sup>I-labeled Cu-Cy-I ([<sup>131</sup>I]Cu-Cy-I) nanoparticles. <b>Methods</b>: The synthesis of [<sup>131</sup>I]Cu-Cy-I nanoparticles was performed with [<sup>131</sup>I]I<sup>−</sup> anions. The in vitro radiobiological effects on tumor cells incubated with Cu-Cy-I nanoparticles by X-ray irradiation were investigated. The in vivo tumor growth-inhibitory effects of the combination of Cu-Cy-I nanoparticles with X-ray radiotherapy and [<sup>131</sup>I]Cu-Cy-I nanoparticles were evaluated with 4T1 tumor-xenografted mice. <b>Results</b>: The in vitro experiment results indicated that the X-ray irradiation with the presence of Cu-Cy-I nanoparticles produced a higher intracellular reactive oxygen species (ROS) level and more DNA damage of 4T1 cells and showed a stronger tumor cell killing ability compared to X-ray irradiation alone. The in vivo experimental results with 4T1 breast carcinoma-bearing mice showed that the combination of an intratumoral injection of Cu-Cy-I nanoparticles and X-ray radiotherapy enhanced the tumor growth-inhibitory effect and prolonged the mice’s lives. <b>Conclusions</b>: Cu-Cy-I nanoparticles have good potential as new radiosensitizers to enhance the efficacy of external X-ray radiotherapy. However, the efficacy of local treatment with [<sup>131</sup>I]Cu-Cy-I nanoparticles at a low <sup>131</sup>I dose was not verified. The effective synthesis of smaller sizes of nanoparticles is necessary for further investigation of the radiotherapy potential of [<sup>131</sup>I]Cu-Cy-I nanoparticles.
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spelling doaj-art-0b3303f30dbd4befb98afe0ddffcbb232025-08-20T03:12:04ZengMDPI AGPharmaceutics1999-49232025-01-0117214910.3390/pharmaceutics17020149Iodinated Copper–Cysteamine Nanoparticles as Radiosensitizers for Tumor RadiotherapyMiaomiao Zhang0Yu Yang1Ying Xu2Jie Wang3Shihong Li4State Key Laboratory of Radiation Medicine and Protection, School of Radiation Medicine and Protection, Suzhou Medical College of Soochow University, Suzhou 215123, ChinaState Key Laboratory of Radiation Medicine and Protection, School of Radiation Medicine and Protection, Suzhou Medical College of Soochow University, Suzhou 215123, ChinaState Key Laboratory of Radiation Medicine and Protection, School of Radiation Medicine and Protection, Suzhou Medical College of Soochow University, Suzhou 215123, ChinaInstitute for Advanced Materials, School of Material Science and Engineering, Jiangsu University, Zhenjiang 212013, ChinaState Key Laboratory of Radiation Medicine and Protection, School of Radiation Medicine and Protection, Suzhou Medical College of Soochow University, Suzhou 215123, China<b>Background/Objectives:</b> Radiotherapy is a widely applied first-line clinical treatment modality of cancer. Copper–cysteamine (Cu-Cy) nanoparticles represent a new type of photosensitizer that demonstrates significant anti-tumor potential by X-ray-induced photodynamic therapy. Iodide is a high-Z element with superior X-ray absorption ability and has the β-decay radiotherapeutic nuclide, <sup>131</sup>I, which emits Cherenkov light. In this study we aimed to investigate the X-ray-induced photodynamic therapy potential of iodinated Cu-Cy (Cu-Cy-I) nanoparticles and also explore the local treatment efficacy of <sup>131</sup>I-labeled Cu-Cy-I ([<sup>131</sup>I]Cu-Cy-I) nanoparticles. <b>Methods</b>: The synthesis of [<sup>131</sup>I]Cu-Cy-I nanoparticles was performed with [<sup>131</sup>I]I<sup>−</sup> anions. The in vitro radiobiological effects on tumor cells incubated with Cu-Cy-I nanoparticles by X-ray irradiation were investigated. The in vivo tumor growth-inhibitory effects of the combination of Cu-Cy-I nanoparticles with X-ray radiotherapy and [<sup>131</sup>I]Cu-Cy-I nanoparticles were evaluated with 4T1 tumor-xenografted mice. <b>Results</b>: The in vitro experiment results indicated that the X-ray irradiation with the presence of Cu-Cy-I nanoparticles produced a higher intracellular reactive oxygen species (ROS) level and more DNA damage of 4T1 cells and showed a stronger tumor cell killing ability compared to X-ray irradiation alone. The in vivo experimental results with 4T1 breast carcinoma-bearing mice showed that the combination of an intratumoral injection of Cu-Cy-I nanoparticles and X-ray radiotherapy enhanced the tumor growth-inhibitory effect and prolonged the mice’s lives. <b>Conclusions</b>: Cu-Cy-I nanoparticles have good potential as new radiosensitizers to enhance the efficacy of external X-ray radiotherapy. However, the efficacy of local treatment with [<sup>131</sup>I]Cu-Cy-I nanoparticles at a low <sup>131</sup>I dose was not verified. The effective synthesis of smaller sizes of nanoparticles is necessary for further investigation of the radiotherapy potential of [<sup>131</sup>I]Cu-Cy-I nanoparticles.https://www.mdpi.com/1999-4923/17/2/149copper–cysteamine nanoparticlesradiosensitizationradiotherapyX-ray-induced photodynamic therapy<sup>131</sup>I
spellingShingle Miaomiao Zhang
Yu Yang
Ying Xu
Jie Wang
Shihong Li
Iodinated Copper–Cysteamine Nanoparticles as Radiosensitizers for Tumor Radiotherapy
Pharmaceutics
copper–cysteamine nanoparticles
radiosensitization
radiotherapy
X-ray-induced photodynamic therapy
<sup>131</sup>I
title Iodinated Copper–Cysteamine Nanoparticles as Radiosensitizers for Tumor Radiotherapy
title_full Iodinated Copper–Cysteamine Nanoparticles as Radiosensitizers for Tumor Radiotherapy
title_fullStr Iodinated Copper–Cysteamine Nanoparticles as Radiosensitizers for Tumor Radiotherapy
title_full_unstemmed Iodinated Copper–Cysteamine Nanoparticles as Radiosensitizers for Tumor Radiotherapy
title_short Iodinated Copper–Cysteamine Nanoparticles as Radiosensitizers for Tumor Radiotherapy
title_sort iodinated copper cysteamine nanoparticles as radiosensitizers for tumor radiotherapy
topic copper–cysteamine nanoparticles
radiosensitization
radiotherapy
X-ray-induced photodynamic therapy
<sup>131</sup>I
url https://www.mdpi.com/1999-4923/17/2/149
work_keys_str_mv AT miaomiaozhang iodinatedcoppercysteaminenanoparticlesasradiosensitizersfortumorradiotherapy
AT yuyang iodinatedcoppercysteaminenanoparticlesasradiosensitizersfortumorradiotherapy
AT yingxu iodinatedcoppercysteaminenanoparticlesasradiosensitizersfortumorradiotherapy
AT jiewang iodinatedcoppercysteaminenanoparticlesasradiosensitizersfortumorradiotherapy
AT shihongli iodinatedcoppercysteaminenanoparticlesasradiosensitizersfortumorradiotherapy