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

• Main Authors: Janković Drina Lj., Nikolić Nadežda S., Vukadinović Aleksandar A., Petrović Mirjana M., Vranješ-Đurić Sanja D., Lakić Mladen M.
• Format: Article
• Language: English
• Published: Srpsko lekarsko drustvo 2014-01-01
• Series: Hospital Pharmacology
• Subjects: yttrium-90; radiocolloid; particle size; labeling; tumor therapy
• Online Access: http://scindeks-clanci.ceon.rs/data/pdf/2334-9492/2014/2334-94921403138J.pdf
• ISSN: 2334-9492; 2334-9492

Introduction The suitability of 90Y-labeled antimony trisulfide 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 efficiency of 90Y- and 99mTc-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 (filtration analysis). Results 90Y-labeled ATC can be prepared in high yield under investigated conditions Labeling efficiency was >95% and filtration 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 90Y-ATC was quite stable in vitro in human serum. Tissue distribution studies in rats confirmed that the liver and spleen uptake of 90Y-labeled colloid was three-fold lower in comparison with 99mTc-ATC, although the bone uptake was five-fold higher at 20 min post injection. Conclusions 90Y-labeled ATC showed high labeling efficiency and good stability, and might be well suited for therapeutic application in nuclear medicine.