Abstract
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 188W/188Re generator, 188Re can be effectively used to develop a therapeutic radio complex. In this study, 188Re-HYNIC-BBN was prepared under optimal conditions. Optimization of the effective parameters on 188Re-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 188Re-HYNIC-BBN and free 188Re in different organs of the rats were compared in various intervals. 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 = 45min, temp = 95℃). This radio-complex was found to be stable in PBS and blood serum over 24h. LogPo/w was - 1.78, showing the high hydrophilic nature of the radio-complex. The biodistribution of 188Re-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. The special characteristics of the complex introduce 188Re-HYNIC-BBN as a new therapeutic agent for targeting GRPRs, however, more biological data is still needed.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.