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Merck

Delivery of antiviral agents in liposomes.

Methods in enzymology (2005-02-22)
Nejat Düzgüneş, Sergio Simões, Vladimir Slepushkin, Elizabeth Pretzer, Diana Flasher, Isam I Salem, Gerhard Steffan, Krystyna Konopka, Maria C Pedroso de Lima
RÉSUMÉ

The intracellular activity of certain antiviral agents, including antisense oligonucleotides, acyclic nucleoside phosphonates, and protease inhibitors, is enhanced when they are delivered in liposome-encapsulated form. In this chapter we describe the preparation of pH-sensitive liposomes encapsulating antisense oligonucleotides, ribozymes, and acyclic nucleoside phosphonate analogues and their effects on HIV replication in macrophages. We outline the use of liposomal HIV protease inhibitors in infected macrophages. We present two methods for the covalent coupling of soluble CD4 to liposomes and show the association of these liposomes with HIV-infected cells. We also describe the synthesis of a novel antiviral agent based on cyclodextrin and its incorporation into liposomes.

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S-Acetylthioglycolic acid N-hydroxysuccinimide ester, ≥95% (TLC), powder