90Y-labeled antimony trisulfide colloid as promising therapeutic agent: Physicochemical characterization and biological evaluation

Abstract

Introduction The suitability of 90 Y-labeled antimony trisulfi de colloid (ATC) for the preparation of therapeutic radiopharmaceutical was studied taking into accounts its physicochemical properties and biological behavior in rats. Material and methods The labeling effi ciency of 90 Y-and 99 mTc-labeled colloid particles was investigated by ITLC-SG and paper chromatography, the in vitro stability of the colloid was tested in human serum, while in vivo experiments were performed on healthy Wistar rats. Analysis of the particles enclosed the size (TEM), determination of the zeta potential (Zetasizer Nano) as well as radioactivity particle size distribution (fi ltration analysis). Results 90 Y-labeled ATC can be prepared in high yield under investigated conditions Labeling effi ciency was >95% and fi ltration analysis showed that more than 90% of radioactive particles were smaller than 20 nm. The particles with the size range of 6-22 nm were achieved by using polyvinyipyrrolidone (mol wt ~44,000). The 90 Y-ATC was quite stable in vitro in human serum. Tissue distribution studies in rats confi rmed that the liver and spleen uptake of 90 Y-labeled colloid was threefold lower in comparison with 99 mTc-ATC, although the bone uptake was fi ve-fold higher at 20 min post injection. Conclusions 90 Y-labeled ATC showed high labeling effi ciency and good stability, and might be well suited for therapeutic application in nuclear medicine.