A conjugate of lactosaminated poly-L-lysine with adenine arabinoside monophosphate, administered to mice by intramuscular route, accomplishes a selective delivery of the drug to the liver

Biochem Pharmacol. 1994 Feb 11;47(4):643-50. doi: 10.1016/0006-2952(94)90126-0.

Abstract

A conjugate of the antiviral agent adenine arabinoside monophosphate (ara-AMP) with a low molecular mass lactosaminated poly-L-lysine, administered to mice by i.m. route, selectively delivers the drug to the liver. In mice the conjugate is devoid of acute toxicity even at high dose (1.3 mg/g) and injected i.m. for 20 days does not induce antibodies. Moreover it is highly soluble in water; this means that a pharmacologically active dose may be administered in a small volume compatible with the i.m. route. Compared to the similar ara-AMP complex with lactosaminated albumin which must be injected intravenously, the present conjugate might assure a better compliance of patients with hepatitis B virus infection for a long lasting, liver targeted antiviral treatment.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Sugars / pharmacokinetics*
  • Animals
  • Antiviral Agents / administration & dosage*
  • Carbon Radioisotopes
  • Drug Carriers
  • Female
  • Hepatitis B / drug therapy
  • Liver / metabolism*
  • Mice
  • Polylysine / analogs & derivatives*
  • Polylysine / pharmacokinetics*
  • Tissue Distribution
  • Tritium
  • Vidarabine Phosphate / administration & dosage
  • Vidarabine Phosphate / analogs & derivatives*
  • Vidarabine Phosphate / chemistry
  • Vidarabine Phosphate / pharmacokinetics*

Substances

  • Amino Sugars
  • Antiviral Agents
  • Carbon Radioisotopes
  • Drug Carriers
  • lactosaminated polylysine-adenine arabinoside monophosphate
  • Tritium
  • Vidarabine Phosphate
  • lactosamine
  • Polylysine