Coupling of antiviral nucleoside analogs to lactosaminated human albumin by using the imidazolides of their phosphoric esters

Anal Biochem. 1993 Aug 1;212(2):407-11. doi: 10.1006/abio.1993.1348.

Abstract

Liver targeting of antiviral nucleoside analogs can be obtained by conjugating these drugs with the hepatotropic molecule lactosaminated serum albumin. We describe a new coupling procedure which uses the imidazolides of the phosphoric ester derivatives of the drugs in an alkaline medium. By this procedure conjugates are obtained with a high drug/carrier molar ratio and without the unwanted protein chemical changes produced by carbodiimides usually employed for this coupling.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacokinetics
  • Antiviral Agents / pharmacology
  • Chemistry, Pharmaceutical
  • Drug Carriers
  • Drug Stability
  • Electrophoresis, Polyacrylamide Gel
  • Esters / chemical synthesis
  • Humans
  • Hydrogen-Ion Concentration
  • Imidazoles / chemical synthesis*
  • Imidazoles / pharmacokinetics
  • Imidazoles / pharmacology
  • Isoelectric Point
  • Liver / metabolism
  • Magnetic Resonance Spectroscopy
  • Nucleosides / chemical synthesis*
  • Nucleosides / pharmacokinetics
  • Nucleosides / pharmacology
  • Phosphoric Acids / chemical synthesis
  • Phosphorus
  • Rats
  • Serum Albumin / chemical synthesis*
  • Serum Albumin / pharmacology
  • Vidarabine Phosphate / chemical synthesis
  • Vidarabine Phosphate / pharmacokinetics
  • Vidarabine Phosphate / pharmacology

Substances

  • Antiviral Agents
  • Drug Carriers
  • Esters
  • Imidazoles
  • Nucleosides
  • Phosphoric Acids
  • Serum Albumin
  • lactosaminated serum albumin
  • Vidarabine Phosphate
  • Phosphorus