Development and evaluation of 177 Lu-imatinib: radiolabeling and cell culture studies
Makaleler > Tam Makale · 2025
Yazarlar: Emre ÖZGENÇ, Merve Karpuz, Gunnur Guler, Zeynep BURAK, Yücel BAŞPINAR, Evren ATLIHAN GÜNDOĞDU
Radiochimica Acta, Uluslararası, Wos, 2025, cilt 113, ss 899-911
Özet
Abstract Targeted radiopharmaceuticals offer promising approaches for cancer diagnosis and therapy. This study developed freeze-dried kit formulations of 177 Lu-Imatinib (IMT) and evaluated their potential efficacy through in vitro studies. Four formulations (F1–F4) containing IMT and chelating agents were prepared and characterized via Fourier transform infrared (FTIR), ultraviolet spectrum (UV), and thermogravimetric analysis (TGA) to confirm complex formation. Biocompatibility was assessed in NIH-3T3 cells using the MTT assay. Radiolabeling with 177 Lu was optimized by varying pH, incubation time, and reactant ratios. Radiochemical purity and stability were analyzed over 7 days using HPLC. Binding affinity and cytotoxicity were evaluated in MCF-7 and NIH-3T3 cells. Spectroscopic analyses confirm successful complex formation. All formulations exhibited >90 % viability in NIH-3T3 cells. Optimal radiolabeling conditions (45 mg IMT-chelator, pH 5, 60 min incubation) yielded >90 % efficiency, with stable radiolabeling for 7 days. The 177 Lu-IMT-DOTA (F3) formulation showed significantly higher binding and cytotoxic effects in MCF-7 cells compared to controls. The 177 Lu-IMT-DOTA (F3) kit demonstrates high radiolabeling efficiency, stability, and selective in vitro cytotoxicity toward breast cancer cells, supporting its potential as a targeted radiopharmaceutical.