Synthesis and Biological Evaluation of Bisphosphonate Compound Labeled with 99mTc(CO)3

• Published in: Chemical biology & drug design 2015-03, Vol.85 (3), p.369-376
• Main Authors: Şenocak, Kamile, Teksöz, Serap, İçhedef, Çiğdem, Uçar, Eser
• Format: Article
• Language: English
• Subjects: [99mTc(CO)3]+ core; biodistribution; bisphosphonate; DTPA
• ISSN: 1747-0277; 1747-0285
• DOI: 10.1111/cbdd.12401

In this study, radiolabeling of a bisphosphonate, alendronate (Alendronate sodium), was performed with the help of a bifunctional chelating agent. For that purpose, DTPA‐NHS (Diethylenetriaminepentaacetic acid dianhydride‐N‐hydroxysuccinimide) was synthesized with an esterification between DTPA and NHS. Combining the DTPA‐NHS ester with alendronate yields the DTPA‐Alendronate compound. The structure of synthesized compound was analyzed by 1H/13C/31P‐NMR and HPLC. After then, the labeling with [99mTc(CO)3]+ core of synthesized compound was provided. Performing quality controls of newly synthesized [99mTc(CO)3‐DTPA‐Alendronate] complex with thin layer radiochromatography (TLRC) and high‐performance liquid radiochromatography (HPLRC), the labeling yield was found as 99%. It was observed that the compound conserves its stability for 24 h in serum media. Biodistribution of the radiolabeled complex was performed on Wistar Albino rats to determine radiopharmaceutical potential of the [99mTc(CO)3‐DTPA‐Alendronate] complex. It is thought that the data gained from this study will contribute to the development of complexes with bisphosphonate. In the present study a new derivative of alendronate was designed and radiolabeled for imaging purposes. The preparation, characterization and biological evaluation of this newly synthesized 99mTc(CO)3‐Diethylenetriaminepentaacetic acid‐Alendronate (99mTc(CO)3‐DTPA‐ABP) complex was performed. Biological evaluation of the radiolabelled complex was performed by biodistribution studies on female rats.