Optimized Production of 188 Re-HYNIC-Bombesin: New Therapeutic Agent for GRPR Targeting.

Autor: Vosoughi S; Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Box 14395‑836, North Kargar Street, Tehran, Iran., Salek N; Nuclear Fuel Research School, Nuclear Science and Technology Research Institute (NSTRI), Box 14395‑836, North Kargar Street, Tehran, Iran., Zolghadri S; Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Box 14395‑836, North Kargar Street, Tehran, Iran., Aghamiri SMR; Department of Radiation Medicine Engineering, Shahid Beheshti University, Tehran, Iran., Delavari M; Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Box 14395‑836, North Kargar Street, Tehran, Iran.
Jazyk: angličtina
Zdroj: Nuclear medicine and molecular imaging [Nucl Med Mol Imaging] 2024 Aug; Vol. 58 (5), pp. 300-309. Date of Electronic Publication: 2024 Jun 01.
DOI: 10.1007/s13139-024-00866-1
Abstrakt: Purpose: One of the most interesting methods to deliver therapeutic doses of ionizing radiation to tumor sites is radiolabeled compounds. Bombesin peptide binds to gastrin-releasing peptide receptors (GRPRs) with great affinity. Through its appropriate physical characteristics and accessibility as the 188 W/ 188 Re generator, 188 Re can be effectively used to develop a therapeutic radio complex. In this study, 188 Re-HYNIC-BBN was prepared under optimal conditions.
Methods: Optimization of the effective parameters on 188 Re-HYNIC-BBN radio-labeling yield like ligand concentration, pH, reaction time, and temperature were performed. The final product's radiochemical purity was measured by RTLC and HPLC. The stability of the radio-complex was checked in PBS buffer (4 °C) and human blood serum (37 °C). The partition coefficient of the final radio-complex was studied using standard procedure. Finally, the biodistribution of 188 Re-HYNIC-BBN and free 188 Re in different organs of the rats were compared in various intervals.
Results: The final product was prepared with a specific activity of 7.11 TBq/mmol and radiochemical purity > 95% at the optimized conditions (pH = 4-5, reaction time = 45 min, temp = 95℃). This radio-complex was found to be stable in PBS and blood serum over 24 h. LogP o/w was - 1.78, showing the high hydrophilic nature of the radio-complex. The biodistribution of 188 Re-HYNIC-BBN demonstrated the fast clearance of the radio-peptide from the blood circulation. The most portion of the radioactivity was excreted from the body via the urinary tract and the remaining activity was accumulated in GRPR-expressing organs.
Conclusion: The special characteristics of the complex introduce 188 Re-HYNIC-BBN as a new therapeutic agent for targeting GRPRs, however, more biological data is still needed.
Competing Interests: Competing InterestsSara Vosoughi, Nafise Salek, Samaneh Zolghadri, Seyed Mahmoud Reza Aghamiri, and Milad Delavari declare that they have no competing interests.
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Databáze: MEDLINE
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