Synthesis, Characterization, and Therapeutic Efficacy of 177 Lu-DMSA@SPIONs in Nanobrachytherapy of Solid Tumors.
In: Pharmaceutics, Jg. 15 (2023-07-01), Heft 7, S. 1943-1959
Online
academicJournal
Zugriff:
As an alternative to classical brachytherapy, intratumoral injection of radionuclide-labeled nanoparticles (nanobrachytherapy, NBT) has been investigated as a superior delivery method over an intravenous route for radionuclide therapy of solid tumors. We created superparamagnetic iron oxide nanoparticles (SPIONs) coated with meso-1,2-dimercaptosuccinic acid (DMSA) and radiolabeled with Lutetium-177 (177Lu), generating 177Lu-DMSA@SPIONs as a potential antitumor agent for nanobrachytherapy. Efficient radiolabeling of DMSA@SPIONS by 177Lu resulted in a stable bond with minimal leakage in vitro. After an intratumoral injection to mouse colorectal CT-26 or breast 4T1 subcutaneous tumors, the nanoparticles remained well localized at the injection site for weeks, with limited leakage. The dose of 3.70 MBq/100 µg/50 µL of 177Lu-DMSA@SPIONs applied intratumorally resulted in a high therapeutic efficacy, without signs of general toxicity. A decreased dose of 1.85 MBq/100 µg/50 µL still retained therapeutic efficacy, while an increased dose of 9.25 MBq/100 µg/50 µL did not significantly benefit the therapy. Histopathology analysis revealed that the 177Lu-DMSA@SPIONs act within a limited range around the injection site, which explains the good therapeutic efficacy achieved by a single administration of a relatively low dose without the need for increased or repeated dosing. Overall, 177Lu-DMSA@SPIONs are safe and potent agents suitable for intra-tumoral administration for localized tumor radionuclide therapy. [ABSTRACT FROM AUTHOR]
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Synthesis, Characterization, and Therapeutic Efficacy of 177 Lu-DMSA@SPIONs in Nanobrachytherapy of Solid Tumors.
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Autor/in / Beteiligte Person: | Stanković, Dragana ; Radović, Magdalena ; Stanković, Aljoša ; Mirković, Marija ; Vukadinović, Aleksandar ; Mijović, Milica ; Milanović, Zorana ; Ognjanović, Miloš ; Janković, Drina ; Antić, Bratislav ; Vranješ-Đurić, Sanja ; Savić, Miroslav ; Prijović, Željko |
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Zeitschrift: | Pharmaceutics, Jg. 15 (2023-07-01), Heft 7, S. 1943-1959 |
Veröffentlichung: | 2023 |
Medientyp: | academicJournal |
ISSN: | 1999-4923 (print) |
DOI: | 10.3390/pharmaceutics15071943 |
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