Synthesis, radiolabeling and bioevaluation of 99mTc (CO)3-folate azide complex for tumor detection. | [Journal of Chemical Society of Pakistan • 2013]

Author(s):

1. Irfanullah Khan: Radiopharmacy and PET Radiochemistry Division, Institute of Nuclear Medicine & Oncology (INMOL), Lahore, Pakistan

2. Abubaker Shahid: Radiopharmacy and PET Radiochemistry Division, Institute of Nuclear Medicine & Oncology (INMOL), Lahore, Pakistan

3. Fayyaz Ahmad: Radiopharmacy and PET Radiochemistry Division, Institute of Nuclear Medicine & Oncology (INMOL), Lahore, Pakistan

4. Ume Kalsoom Dar: Radiopharmacy and PET Radiochemistry Division, Institute of Nuclear Medicine and Oncology (INMOL), Lahore, Pakistan; Institute of Chemistry, University of the Punjab, Lahore, Pakistan

5. Ijazullah Khan: Institute of Chemistry, University of the Punjab, Lahore, Pakistan

6. Muhammad Javed: Gujranwala Institute of Nuclear Medicine (GINUM), Gujranwala, Pakistan

7. Mahera Roohi: Gujranwala Institute of Nuclear Medicine (GINUM), Gujranwala, Pakistan

Abstract:

Folic acid is a common dietary vitamin. Various cancer lines exhibit folate receptors on their surface. Many studies have been carried out to radiolabel the folic acid for diagnostic and therapeutic study of tumor. The aim of the present work is to develop 99mTc(CO)3-folate azide complex for tumor scintigraphy. 1,2,3-Triazole-containing folate azide complex was synthesized by using click chemistry strategy. The product was characterized by matrix-assisted LASER desorption ionization (MALDI). The radiolabeling was carried out by using isolink kit for stable complexation of organometallic core with folate azide complex. The radiochemical purity of the product was observed by using paper chromatography (PC). The protein binding assay in human blood was also studied. Normal distribution and tumoral uptake study of the drug was carried out in Swiss Webster mice. MALDI data showed molecule ion peak of the folate azide complex at m/z 636.279, which confirmed the successful synthesis of the ligand. Radiochemical analysis showed 98.2 ± 1.6 % binding of radiometal with the ligand, which remained >96% up to 5h. Drug showed 70.1 ± 2.8 % binding with blood plasma proteins. Biodistribution results exhibited high uptake in targeted tumor and significantly low accumulation in non targeted organs. These data indicate that 99mTc(CO)3-folate azide complex might prove a successful tumor scintigraphic agent in future clinical applications.

Page(s): 1584-1589

DOI: DOI not available

Published: Journal: Journal of Chemical Society of Pakistan, Volume: 35, Issue: 6, Year: 2013

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