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.
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.
Fiume
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L
Dipartimento di Patologia Sperimentale, Università di Bologna, Italy.
Di Stefano
G
G
Busi
C
C
Mattioli
A
A
D000606:Amino Sugars / Q000493:pharmacokinetics*; D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage*; D002250:Carbon Radioisotopes; D004337:Drug Carriers; D005260:Female; D006509:Hepatitis B / Q000188:drug therapy; D008099:Liver / Q000378:metabolism*; D051379:Mice; D011107:Polylysine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D014316:Tritium; D001084:Vidarabine Phosphate / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics*
D000606:Amino Sugars; D000998:Antiviral Agents; D002250:Carbon Radioisotopes; D004337:Drug Carriers; C086198:lactosaminated polylysine-adenine arabinoside monophosphate; D014316:Tritium; D001084:Vidarabine Phosphate; C032233:lactosamine; D011107:Polylysine