Evaluation Efficacy of Rhenium-188-Loaded Micro-particles for Radiotherapy in a Mouse Model of Hepatocellular Carcinoma

Mol Pharm. 2019 Mar 4;16(3):1083-1091. doi: 10.1021/acs.molpharmaceut.8b01083. Epub 2019 Feb 1.

Abstract

Hepatocellular carcinoma (HCC) is one of the leading causes of mortality worldwide. The aim of the present study was to evaluate the distribution and the therapeutic effect of 188Re-Tin-colloid micro-particles in subcutaneous HCC-bearing mice. The synthesis and characterization of micro-particles labeled with the 188Re isotope were performed. The micro-particles were injected into the tumor site subcutaneously in the BNL HCC-bearing mice with three treatment groups, normal saline, 188Re micro-particles, and 188Re-Tin-colloid micro-particles. The results of biodistribution showed that major radioactivity (188Re) of 188Re-Tin-colloid micro-particles (18.69 ± 4.28 %ID/g) remained at the tumor sites, compared with 188Re micro-particles (0.21 ± 0.12 %ID/g), 24 h post injection. Following the injection of 188Re-Tin-colloid micro-particles for 14 days, all BNL tumors in mice were regressed during the observation period. By contrast, all of the mice treated with normal saline or 188Re micro-particles had died by 24 and 28 days, respectively. The 188Re-Tin-colloid micro-particles demonstrated high accumulation and therapeutic potential in the subcutaneous HCC-bearing mice.

Keywords: 188Re; colloid; hepatocellular carcinoma; micro-particles.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism*
  • Antineoplastic Agents / therapeutic use*
  • Carcinoma, Hepatocellular / radiotherapy*
  • Cell Line, Tumor
  • Colloids / chemistry
  • Disease Models, Animal
  • Drug Compounding / methods
  • Drug Delivery Systems
  • Liver Neoplasms / radiotherapy*
  • Mice
  • Mice, Inbred BALB C
  • Microspheres*
  • Particle Size
  • Radioisotopes / chemistry
  • Radioisotopes / metabolism*
  • Radioisotopes / therapeutic use*
  • Radiopharmaceuticals / therapeutic use*
  • Rhenium / chemistry
  • Rhenium / metabolism*
  • Rhenium / therapeutic use*
  • Single Photon Emission Computed Tomography Computed Tomography
  • Tin Compounds / chemistry
  • Tissue Distribution
  • Treatment Outcome
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Colloids
  • Radioisotopes
  • Radiopharmaceuticals
  • Tin Compounds
  • stannous chloride
  • Rhenium-188
  • Rhenium