       Document 0791
 DOCN  M9610791
 TI    Lymphoid tissues targeting of liposome-encapsulated
       2',3'-dideoxyinosine.
 DT    9601
 AU    Harvie P; Desormeaux A; Gagne N; Tremblay M; Poulin L; Beauchamp D;
       Bergeron MG; Centre de Recherche en Infectiologie, Centre Hospitalier
       de; l'Universite Laval, Ste-Foy, Quebec, Canada.
 SO    AIDS. 1995 Jul;9(7):701-7. Unique Identifier : AIDSLINE MED/96035232
 AB    OBJECTIVE: To improve the pharmacokinetics and lymphoid tissues
       targeting of 2',3'-dideoxyinosine (ddI) by encapsulation in liposomes.
       METHODS: The pharmacokinetics and tissue distribution of free and
       liposome-encapsulated ddI were determined in C57BL/6 mice following
       intravenous and subcutaneous administration of a single bolus dose (3 mg
       ddI/kg). RESULTS: Intravenous administration of liposome-encapsulated
       ddI greatly reduced the systemic clearance of the anti-HIV agent. The
       elimination plasma half-life of ddI incorporated in 112 and 83 nm
       liposomes was 46 and 14 times higher than that of the free drug,
       respectively. The tissue distribution profile of liposomal lipids
       clearly showed that the use of liposomes allows efficient targeting of
       lymph nodes and macrophage-rich tissues (spleen and liver) for at least
       24 h following intravenous injection. In contrast, the accumulation of
       liposomes in these tissues was much lower following subcutaneous
       administration. CONCLUSION: Incorporation of ddI in liposomes greatly
       improved the pharmacokinetics of the anti-HIV agent after intravenous
       injection. The use of liposomes could represent a convenient approach to
       targeting lymphoid tissues. Strategies aimed at improving drug retention
       within liposomes should further enhance and prolong drug delivery to
       lymphoid organs.
 DE    Animal  Antiviral Agents/*ADMINISTRATION & DOSAGE/PHARMACOKINETICS
       Didanosine/*ADMINISTRATION & DOSAGE/PHARMACOKINETICS  Drug Carriers
       HIV/DRUG EFFECTS  Injections, Intravenous  Injections, Subcutaneous
       Liposomes  Lymphoid Tissue/*DRUG EFFECTS/VIROLOGY  Mice  Mice, Inbred
       C57BL  Support, Non-U.S. Gov't  Tissue Distribution  JOURNAL ARTICLE

       SOURCE: National Library of Medicine.  NOTICE: This material may be
       protected by Copyright Law (Title 17, U.S.Code).

