90Y-labeled tin fluoride colloid as a promising therapeutic agent: preparation, characterization, and biological study in rats

J Pharm Sci. 2012 Jun;101(6):2194-203. doi: 10.1002/jps.23114. Epub 2012 Mar 13.

Abstract

In this study, tin fluoride colloid (SnF-c) was prepared, labeled with yttrium-90 ((90)Y), and characterized with respect to its physicochemical properties and biological behavior in an animal model. Particle size of SnF-c, at constant concentration of SnF(2), was dependent on pH, concentration of sodium fluoride (NaF), temperature, and time. The particle size of SnF-c decreased with an increase in NaF concentration and a decrease in reaction mixture pH. Radiolabeling yield of (90)Y-SnF-c at higher temperature increased and it was greater than 98% for the preparation at 95 °C. The (90)Y-SnF-c demonstrated high in vitro stability both in human serum and human synovial fluid at 37 °C up to 7 days. In vivo distribution studies in healthy male Wistar rats of (90)Y-SnF-c (particles <1 μm), following intravenous administration, revealed that the localization takes place preferably in the liver. The (90)Y-SnF-c (particles >1 μm) was well retained in the synovial space for 96 h after intra-articular injection, whereas leakage of (90)Y from the joint was 1.96% over this period. Because of high labeling yield and stability, (90)Y-SnF-c might be a promising agent for radiosynovectomy or therapy of liver malignancies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Colloids*
  • Male
  • Microscopy, Electron, Scanning
  • Particle Size
  • Rats
  • Rats, Wistar
  • Tin Fluorides / chemistry*
  • Tin Fluorides / pharmacokinetics
  • Tissue Distribution
  • Yttrium Radioisotopes / chemistry*
  • Yttrium Radioisotopes / pharmacokinetics

Substances

  • Colloids
  • Tin Fluorides
  • Yttrium Radioisotopes