ArticleMolecular pharmaceutics2026
Auger Electron Therapy Enhanced by Heat-Triggered Release of I-125-Labeled DNA-Targeted Compounds within the Tumor Microenvironment.
Article in Molecular pharmaceutics, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
In Auger electron therapy, the effective delivery of Auger electron-emitting radionuclides to the nuclei of cancer cells is essential for achieving high therapeutic efficacy. In this study, we developed a novel strategy that combined thermosensitive liposomes (TSLs) encapsulating 125I-labeled DNA-targeted compounds. This approach enabled enhanced tumor accumulation via TSL-mediated delivery and efficient nuclear translocation of radioactivity by releasing an 125I-labeled doxorubicin derivative ([125I]I-DOX) within the tumor microenvironment. [125I]I-DOX exhibited high cellular and nuclear uptake, producing potent cytotoxicity through Auger electrons emitted from 125I. [125I]I-DOX-loaded TSLs efficiently released [125I]I-DOX at 43 °C, enhancing its cellular uptake by Colon-26 cells. Tumor accumulation of radioactivity in the heating group was much higher than in the nonheating group, and the accumulation was maintained for up to 48 h postinjection. Intravenous injection of [125I]I-DOX-loaded TSLs (5.0 MBq) and localized tumor heating significantly inhibited tumor growth without body weight loss. The combination of [125I]I-DOX-loaded TSLs and hyperthermia represents a promising strategy for Auger electron therapy targeting the nuclei of cancer cells.
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