Production and characterization of 166Ho polylactic acid microspheres

J Labelled Comp Radiopharm. 2016 Jan;59(1):24-9. doi: 10.1002/jlcr.3366. Epub 2015 Dec 22.

Abstract

Microsphere and particle technology with selective transport of radiation represents a new generation of therapeutics. Poly-L-lactic acid (PLLA) microspheres loaded with holmium-166 acetylacetonate ((166)Ho-PLLA-MS) are novel microdevices. In this research, (165)HoAcAc-PLLA microparticles were prepared by the solvent evaporation technique. Microspheres were irradiated at Tehran Research Reactor. The diameter and surface morphologies were characterized by particle sizer and scanning electron microscopy before and after irradiation. The complex stability, radiochemical purity, and in vivo biodistribiotion were checked in the final solution up to 3 days. In this study, (166)Ho-PLLA spherical particles with a smooth surface and diameter of 20-40 µm were obtained, which were stable in vitro and in vivo studies. Neutron irradiation did not damage the particles. The ease with which the PLLA spheres could be made in the optimal size range for later irradiation and their ability to retain the (166)Ho provided good evidence for their potential use in radioembolization.

Keywords: drug delivery; holmium-166; poly-l-lactic acid (PLLA); radioembolization.

MeSH terms

  • Animals
  • Holmium / chemistry*
  • Hydroxybutyrates / chemistry
  • Lactic Acid / chemistry*
  • Microspheres*
  • Pentanones / chemistry
  • Polyesters
  • Polymers / chemistry*
  • Radioisotopes / chemistry
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacokinetics
  • Rats
  • Tissue Distribution

Substances

  • Hydroxybutyrates
  • Pentanones
  • Polyesters
  • Polymers
  • Radioisotopes
  • Radiopharmaceuticals
  • acetyl acetonate
  • Lactic Acid
  • poly(lactide)
  • Holmium