Objectives: To observe the bio-distribution and change in blood kinetics of iron chelating drug-desferrioxamine covalently bound to high-molecular weight dialdehyde cellulose. Methods/Statistical Analysis: The DAC-DFO conjugate and free desferrioxamine were labeled with radiotracer 99mTc. In vitro studies, to establish quality control parameters, were performed by instant thin layer chromatography followed by intravenous administration of radio complexes to the rabbits. Gamma camera imaging was carried out and bio-distribution parameters of both conjugate and free drug were evaluated and compared. Findings: Both polymers based and free desferrioxamine samples exhibited > 90% radiolabelling efficiency and a high in-vitro stability. There was significant improvement in blood circulation time after covalent binding of DFO to DAC (at 1500 min) compared to free DFO (at 900 min) After a single injection of 99mTc-DAC-DFO, the highest distribution was observed in the liver at 19.5 minutes with lower uptake in kidneys and urinary bladder till 30min. On the other hand, the highest distribution of free DFO in liver was highest at only 1 minute post-administration. Application/Improvements: The bioavailability of desferrioxamine was found to be enhanced upto several folds after conjugation to oxidized cellulose.
Keywords
99mtc Labeling, Biodistribution, Desferrioxamine, Dialdehyde Cellulose, Scintigraphy
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