Development of Systems for Delivery of Antiviral Drugs
Technical Report,30 Sep 1987,29 Sep 1988
SOUTHERN RESEARCH INST BIRMINGHAM AL BIRMINGHAM United States
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Ribavirin, a broad-spectrum antiviral agent with potent activity in vitro against a number of important RNA viruses of military significance, is severely limited in its usefulness against virus-induced encephalitic diseases because it does not cross the blood-brain barrier will enough to achieve effective antiviral concentrations in the brain. Our efforts are directed toward the brain-specific delivery of ribavirin and other antiviral agents by means of a redox prodrug concept. The scope of the research program involves the synthesis of CNS-targeted prodrug esters of ribavirin and selenazole, pharmacokinetic studies of drug distribution and sustained delivery of drug in the brain, and the evaluation of the therapeutic efficacy of these antiviral prodrugs compared with the parent drugs in the treatment of lethal Venezuelan equine encephalitis VEE, virus and Japanese encephalitis JE virus infections in mice. Antiviral drugs Ribavirin Japanese encephalitis Prodrug esters Brain-specific drug targeting Drug delivery RA 1.