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

Makaleler > Tam Makale · 2011

Yazarlar: Mehmet Onursal, Fatma YURT, Aykut Ozgur

INTERNATIONAL JOURNAL OF PHARMACEUTICS, SCI Expanded İndekslerine Giren Dergi, Uluslararası, 2011, cilt 416, ss 288-292

DOI: 10.1016/j.ijpharm.2011.07.010

Özet

The aim of the present study was to prepare Tc-99m-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 H-1 NMR and LC-MS/MS methods. Folate-glucaric acid was labeled with Tc-99m, and its radiolabelling efficiency was found as 96 +/- 2.0%. Biodistribution study of Tc-99m-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 Tc-99m-folate-glucaric acid indicated high uptake in folate receptor rich tissues such as breast, ovary and uterus. Therefore, Tc-99m-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. (C) 2011 Elsevier B.V. All rights reserved.

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