Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
Permanent URI for this collectionhttps://hdl.handle.net/11147/7148
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Article Development and Evaluation of 177Lu-Imatinib: Radiolabeling and Cell Culture Studies(Walter de Gruyter GmbH, 2025) Ozgenc, E.; Karpuz, M.; Guler, G.; Burak, Z.; Başpainar, Y.; Gundogdu, E.A.Targeted radiopharmaceuticals offer promising approaches for cancer diagnosis and therapy. This study developed freeze-dried kit formulations of 177Lu-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 177Lu 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 (45mg IMT-chelator, pH 5, 60min incubation) yielded >90% efficiency, with stable radiolabeling for 7 days. The 177Lu-IMT-DOTA (F3) formulation showed significantly higher binding and cytotoxic effects in MCF-7 cells compared to controls. The 177Lu-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. © 2025 Walter de Gruyter GmbH, Berlin/Boston 2025.Article Citation - Scopus: 13Her2-Targeted, Degradable Core Cross-Linked Micelles for Specific and Dual Ph-Sensitive Dox Release(John Wiley and Sons Inc, 2022) Bayram, N.N.; Ulu, G.T.; Topuzoğulları, M.; Baran, Y.; Dinçer, İşoğlu, S.Here, a targeted, dual-pH responsive, and stable micelle nanocarrier is designed, which specifically selects an HER2 receptor on breast cancer cells. Intracellularly degradable and stabilized micelles are prepared by core cross-linking via reversible addition−fragmentation chain-transfer (RAFT) polymerization with an acid-sensitive cross-linker followed by the conjugation of maleimide–doxorubicin to the pyridyl disulfide-modified micelles. Multifunctional nanocarriers are obtained by coupling HER2-specific peptide. Formation of micelles, addition of peptide and doxorubicin (DOX) are confirmed structurally by spectroscopical techniques. Size and morphological characterization are performed by Zetasizer and transmission electron microscope (TEM). For the physicochemical verification of the synergistic acid-triggered degradation induced by acetal and hydrazone bond degradation, Infrared spectroscopy and particle size measurements are used. Drug release studies show that DOX release is accelerated at acidic pH. DOX-conjugated HER2-specific peptide-carrying nanocarriers significantly enhance cytotoxicity toward SKBR-3 cells. More importantly, no selectivity toward MCF-10A cells is observed compared to HER2(+) SKBR-3 cells. Formulations cause apoptosis depending on Bax and Caspase-3 and cell cycle arrest in G2 phase. This study shows a novel system for HER2-targeted therapy of breast cancer with a multifunctional nanocarrier, which has higher stability, dual pH-sensitivity, selectivity, and it can be an efficient way of targeted anticancer drug delivery. © 2021 Wiley-VCH GmbH