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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Nanoformulation of antiretroviral drugs enhances their penetration across the blood brain barrier in mice
Nanomedicine: Nanotechnology, Biology, and Medicine, Volume 11, No. 6, Year 2015
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Description
Eradication of virus by sanctuary sites is a main goal in HIV management. The central nervous system (CNS) is a classic model of sanctuary where viral replication occurs despite a complete viral suppression in peripheral blood. In recent years, nanotechnologies have provided a great promise in the eradication of HIV from the CNS. We hereby demonstrate for the first time that the structurally complex antiretroviral drug enfuvirtide (Enf), which normally is unable to penetrate the cerebrospinal fluid, is allowed to cross the blood brain barrier (BBB) in mice by conjugation with a nanoconstruct. Iron oxide nanoparticles coated with an amphiphilic polymer increase Enf translocation across the BBB in both in vitro and in vivo models. The mechanism involves the uptake of nanoconjugated-Enf in the endothelial cells, the nanocomplex dissociation and the release of the peptide, which is eventually excreted by the cells in the brain parenchyma. From the Clinical Editor: Despite the success of cocktail therapy of antiretroviral drugs, the complete eradication of HIV remains elusive, due to existence of viral sanctuary sites. The authors showed in this study that an antiretroviral drug complexed with iron oxide nanoparticles and coated with PMA amphiphilic polymer crosses the blood brain barrier. Furthermore, there was significant anti-viral activity. The results would aid further drug designs to eradicate HIV. © 2015 Elsevier Inc.
Authors & Co-Authors
Mazzucchelli, Serena
Italy, Milan
Ospedale Luigi Sacco - Polo Universitario
Nebuloni, Manuela
Italy, Milan
Università Degli Studi Di Milano
Capetti, Amedeo Ferdinando
Italy, Milan
Ospedale Luigi Sacco - Polo Universitario
Rizzardini, Giuliano
Italy, Milan
Ospedale Luigi Sacco - Polo Universitario
Statistics
Citations: 57
Authors: 4
Affiliations: 4
Identifiers
Doi:
10.1016/j.nano.2015.03.009
ISSN:
15499634
Research Areas
Infectious Diseases