Synthesis and application of lactosylated, 99mTc chelating albumin for measurement of liver function

Bioconjug Chem. 2010 Apr 21;21(4):589-96. doi: 10.1021/bc900275f.

Abstract

Neogalactosylated and neolactosylated albumins are currently used as radiopharmaceutical agents for imaging the liver asialoglycoprotein receptors, which allows the quantification of hepatic liver function in various diseases and also in healthy liver transplant donors. We developed an original process for synthesizing a chelating neolactosylated human albumin using maleimidopropyl-lactose and maleimidopropyl-diethylene triamine pentaacetic acid (DTPA) derivatives. The lactosylated protein (LACTAL) conjugate showed excellent liver uptake compared to nonlactosylated protein and a very high signal-to-noise ratio, based on functional assessment of biodistribution in mice using (99m)Tc-scintigraphy.

MeSH terms

  • Animals
  • Chelating Agents / chemical synthesis
  • Chelating Agents / chemistry
  • Chelating Agents / pharmacokinetics*
  • Humans
  • Liver / diagnostic imaging*
  • Liver / physiology*
  • Liver Function Tests
  • Male
  • Mice
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / pharmacokinetics*
  • Rats
  • Rats, Wistar
  • Serum Albumin / chemical synthesis
  • Serum Albumin / chemistry
  • Serum Albumin / pharmacokinetics*
  • Technetium Tc 99m Aggregated Albumin / chemistry
  • Technetium Tc 99m Aggregated Albumin / pharmacokinetics*
  • Tissue Distribution

Substances

  • Chelating Agents
  • Radiopharmaceuticals
  • Serum Albumin
  • Technetium Tc 99m Aggregated Albumin
  • lactosylated serum albumin