Cell specific uptake of antiretroviral drugs: AZT coupled to LDL inhibits HIV replication in human macrophages
Mankertz, J.; von Baeyer, H.; Rokos, K.; Nündel, M.; Pauli, G.; Riedel, E.
International Journal of Clinical Pharmacology and Therapeutics 33(2): 85-88
1995
ISSN/ISBN: 0946-1965 PMID: 7757316 Document Number: 448684
Macrophages, besides helper T-lymphocytes, are target cells for the human immunodeficiency virus (HIV). We report on a mechanism to deliver selectively antiretroviral drugs to cells of the monocyte/macrophage lineage. These cells and cells of the endothelium express scavenger receptors which mediate the transport of modified low density lipoprotein (LDL). LDL modified by covalently bound azidothymidine (AZT), a potent inhibitor of HIV replication, is internalized via this pathway into human macrophages. Treatment of HIV-1 infected human macrophages with AZT-LDL showed in vitro efficient inhibition of viral replication. In contrast, HIV replication in T-lymphocytes (Molt 4/8), which do not express scavenger receptors, is not inhibited by AZT-LDL but by free AZT.