biostudies-literatureElghobary MENJapan Society for the Promotion of Science1864https://www.ebi.ac.uk/biostudies/studies/S-EPMC9962004biostudies-literatureUnknown28(4)Auger electrons (AEs) are very low-energy electrons emitted by radionuclides such as I-125 (¹²⁵I). This energy is deposited across a small distance (<0.5 μm), resulting in high linear energy transfer that is potent for causing lethal damage to cancer cells. Thus, AE-emitting radiotherapeutic agents have great potential for cancer treatment. In this study, thermosensitive liposomes (TSLs) encapsulating ¹²⁵I-labeled doxorubicin (DOX) derivatives were developed for Auger electron therapy, targeting the DNA of cancer cells. A radioiodinated DOX derivative [¹²⁵I]<b>5</b> highly accumulated in the nuclei of cancer cells and showed potent cytotoxicity against Colon 26 cancer cells by AEs. Subsequently, [¹²⁵I]<b>5</b> was loaded into the TSLs with high eMolecules (Basel, Switzerland)Preparation and Evaluation of Thermosensitive Liposomes Encapsulating I-125-Labeled Doxorubicin Derivatives for Auger Electron Therapy.PMC996200422K07812Mishiro KOgawa KFuchigami TElghobary MENMunekane MfalsePreparation and Evaluation of Thermosensitive Liposomes Encapsulating I-125-Labeled Doxorubicin Derivatives for Auger Electron Therapy.Auger electrons (AEs) are very low-energy electrons emitted by radionuclides such as I-125 (¹²⁵I). This energy is deposited across a small distance (<0.5 μm), resulting in high linear energy transfer that is potent for causing lethal damage to cancer cells. Thus, AE-emitting radiotherapeutic agents have great potential for cancer treatment. In this study, thermosensitive liposomes (TSLs) encapsulating ¹²⁵I-labeled doxorubicin (DOX) derivatives were developed for Auger electron therapy, targeting the DNA of cancer cells. A radioiodinated DOX derivative [¹²⁵I]<b>5</b> highly accumulated in the nuclei of cancer cells and showed potent cytotoxicity against Colon 26 cancer cells by AEs. Subsequently, [¹²⁵I]<b>5</b> was loaded into the TSLs with high e2023-01-01T00:00:00Z2023 Feb2025-04-04T08:53:07.172Z2025-04-04T08:53:07.172ZS-EPMC99620043683885110.3390/molecules28041864