Synthesis and biological evaluation of receptor-based tumor imaging agent: (99m)Tc-folate-glucaric acid.

Mehmet Onursal, Fatma Yurt Lambrecht, Aykut Ozgur

Department of Nuclear Applications, Ege University, Bornova 35100 Izmir, Turkey.

International journal of pharmaceutics 2011 Sep 15

filter terms:

The aim of the present study was to prepare (99m)Tc-folate-glucaric acid and investigate the radiopharmaceutical potential for tumors imaging that over express folate receptor. Folate-glucaric acid was synthesized and the synthesized folate conjugate was confirmed with (1)H NMR and LC-MS/MS methods. Folate-glucaric acid was labeled with (99m)Tc, and its radiolabelling efficiency was found as 96 ± 2.0%. Biodistribution study of (99m)Tc-folate-glucaric acid was carried out in vivo using two groups of female Albino Wistar rats: folate receptor (FR) saturated and unsaturated. Biodistribution study showed that (99m)Tc-folate-glucaric acid indicated high uptake in folate receptor rich tissues such as breast, ovary and uterus. Therefore, (99m)Tc-folate-glucaric acid shows good radiolabeling and biodistribution in FR organs, the radiolabeled conjugate is a reason potentially useful radiopharmaceutical for detection of FR-positive tumors. Copyright © 2011 Elsevier B.V. All rights reserved.

Citation

Mehmet Onursal, Fatma Yurt Lambrecht, Aykut Ozgur. Synthesis and biological evaluation of receptor-based tumor imaging agent: (99m)Tc-folate-glucaric acid. International journal of pharmaceutics. 2011 Sep 15;416(1):288-92