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.

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.

• Authors: L Fiume, G Di Stefano, C Busi, A Mattioli
• Journal: Biochemical pharmacology (Biochem Pharmacol) Vol. 47 Issue 4 Pg. 643-50 (Feb 11 1994) ISSN: 0006-2952 [Print] England
• PMID: 7510478 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

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

Topics

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