Radiolabeling, quality control, and in vitro cell culture studies of [ 99m Tc]Tc-tamoxifen citrate for estrogen receptor-positive breast cancer imaging.
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| Titel: | Radiolabeling, quality control, and in vitro cell culture studies of [ 99m Tc]Tc-tamoxifen citrate for estrogen receptor-positive breast cancer imaging. |
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| Autoren: | Okşaş H; Department of Radiopharmacy, Faculty of Pharmacy, Ege University, Izmir, Türkiye., Ekinci M; Department of Radiopharmacy, Faculty of Pharmacy, Ege University, Izmir, Türkiye. Electronic address: meliha.ekinci@ege.edu.tr. |
| Quelle: | Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine [Appl Radiat Isot] 2025 Nov; Vol. 225, pp. 112023. Date of Electronic Publication: 2025 Jul 03. |
| Publikationsart: | Journal Article |
| Sprache: | English |
| Info zur Zeitschrift: | Publisher: Pergamon Press Country of Publication: England NLM ID: 9306253 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1872-9800 (Electronic) Linking ISSN: 09698043 NLM ISO Abbreviation: Appl Radiat Isot Subsets: MEDLINE |
| Imprint Name(s): | Original Publication: Oxford ; New York : Pergamon Press, c1993- |
| MeSH-Schlagworte: | Breast Neoplasms*/diagnostic imaging , Breast Neoplasms*/metabolism , Tamoxifen*/pharmacokinetics , Tamoxifen*/chemistry , Tamoxifen*/analogs & derivatives , Receptors, Estrogen*/metabolism , Radiopharmaceuticals*/chemical synthesis , Radiopharmaceuticals*/pharmacokinetics , Organotechnetium Compounds*/pharmacokinetics , Organotechnetium Compounds*/chemical synthesis , Organotechnetium Compounds*/chemistry , Technetium*/chemistry, Humans ; Female ; Isotope Labeling/methods ; Isotope Labeling/standards ; Quality Control ; Cell Line, Tumor ; MCF-7 Cells |
| Abstract: | Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. Background: Early and accurate imaging of estrogen receptor-positive (ER + ) breast cancer remains an unmet need in nuclear medicine. Tamoxifen, a selective estrogen receptor modulator, offers a molecular targeting strategy, yet previous radiolabeling approaches often required elevated temperatures or chelating agents. Purpose: This study aimed to develop and evaluate a simple, chelator-free radiolabeling method for tamoxifen citrate (TC) with technetium-99m ([ 99m Tc]Tc) under mild conditions, without requiring purification, and to assess its physicochemical stability and selective uptake in breast cancer cells. Methods: [ 99m Tc]Tc-TC was synthesized using stannous chloride as a reducing agent at room temperature. Radiochemical purity was assessed by radio thin-layer chromatography (RTLC) and radioelectrophoresis. Stability was examined in saline and cell culture media. Cellular uptake was evaluated in ER + (MCF-7) and ER - (MCF-10A) cell lines. A theoretical coordination model of [ 99m Tc]Tc-TC was also proposed. Results: The most stable [ 99m Tc]Tc-TC complex was formed using 0.01 mg of stannous chloride as the reducing agent, 37 MBq of activity at pH 7.4, and a 20 min incubation time. The radiolabeled complex showed >97 % radiochemical purity and remained stable for 6 h in saline and 2 h in cell medium. Cellular uptake in MCF-7 cells was approximately 72-77 %, more than double that in MCF-10A cells (around 30 %), demonstrating ER + selectivity. Radioelectrophoresis confirmed a distinct migration profile from [ 99m Tc]Tc-citrate, supporting the formation of a [ 99m Tc]Tc-TC complex. Conclusions: [ 99m Tc]Tc-TC was successfully synthesized via a simple room-temperature labeling strategy, showing high stability and ER-specific cell uptake. Although in vivo validation is planned for future studies, this formulation holds promise as a receptor-targeted radiopharmaceutical for breast cancer imaging. (Copyright © 2025 Elsevier Ltd. All rights reserved.) |
| Contributed Indexing: | Keywords: Breast cancer; Cell incorporation; Estrogen receptor targeting; Radiolabeling; Radiopharmaceuticals; Tamoxifen citrate; Technetium-99m; [(99m)Tc]Tc-tamoxifen citrate |
| Substance Nomenclature: | 094ZI81Y45 (Tamoxifen) 0 (Receptors, Estrogen) 0 (Radiopharmaceuticals) 0 (Organotechnetium Compounds) 7440-26-8 (Technetium) |
| Entry Date(s): | Date Created: 20250706 Date Completed: 20250829 Latest Revision: 20250829 |
| Update Code: | 20250903 |
| DOI: | 10.1016/j.apradiso.2025.112023 |
| PMID: | 40618535 |
| Datenbank: | MEDLINE |
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Nájsť tento článok vo Web of Science | Abstract: | Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br />Background: Early and accurate imaging of estrogen receptor-positive (ER <sup>+</sup> ) breast cancer remains an unmet need in nuclear medicine. Tamoxifen, a selective estrogen receptor modulator, offers a molecular targeting strategy, yet previous radiolabeling approaches often required elevated temperatures or chelating agents.<br />Purpose: This study aimed to develop and evaluate a simple, chelator-free radiolabeling method for tamoxifen citrate (TC) with technetium-99m ([ <sup>99m</sup> Tc]Tc) under mild conditions, without requiring purification, and to assess its physicochemical stability and selective uptake in breast cancer cells.<br />Methods: [ <sup>99m</sup> Tc]Tc-TC was synthesized using stannous chloride as a reducing agent at room temperature. Radiochemical purity was assessed by radio thin-layer chromatography (RTLC) and radioelectrophoresis. Stability was examined in saline and cell culture media. Cellular uptake was evaluated in ER <sup>+</sup> (MCF-7) and ER <sup>-</sup> (MCF-10A) cell lines. A theoretical coordination model of [ <sup>99m</sup> Tc]Tc-TC was also proposed.<br />Results: The most stable [ <sup>99m</sup> Tc]Tc-TC complex was formed using 0.01 mg of stannous chloride as the reducing agent, 37 MBq of activity at pH 7.4, and a 20 min incubation time. The radiolabeled complex showed >97 % radiochemical purity and remained stable for 6 h in saline and 2 h in cell medium. Cellular uptake in MCF-7 cells was approximately 72-77 %, more than double that in MCF-10A cells (around 30 %), demonstrating ER <sup>+</sup> selectivity. Radioelectrophoresis confirmed a distinct migration profile from [ <sup>99m</sup> Tc]Tc-citrate, supporting the formation of a [ <sup>99m</sup> Tc]Tc-TC complex.<br />Conclusions: [ <sup>99m</sup> Tc]Tc-TC was successfully synthesized via a simple room-temperature labeling strategy, showing high stability and ER-specific cell uptake. Although in vivo validation is planned for future studies, this formulation holds promise as a receptor-targeted radiopharmaceutical for breast cancer imaging.<br /> (Copyright © 2025 Elsevier Ltd. All rights reserved.) |
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| ISSN: | 1872-9800 |
| DOI: | 10.1016/j.apradiso.2025.112023 |