Lymphoid tissues targeting of liposome-encapsulated 2',3'-dideoxyinosine.

Important note: Information in this article was accurate in 1996. The state of the art may have changed since the publication date.

Lymphoid tissues targeting of liposome-encapsulated 2',3'-dideoxyinosine.

AIDS. 1995 Jul;9(7):701-7. Unique Identifier : AIDSLINE MED/96035232
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.

Abstract: 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.

Keywords: 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

960130
M9610791

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