Abstract
Homo- and heterodimers of nucleoside/nucleotide analogues as reverse transcriptase inhibitors are effective on HIV-1-infected human monocyte-derived macrophages (M/M) compared to the single drugs or their combination. Since the combined treatment of lamivudine (3TC) and tenofovir ((R)PMPA) has an antiretroviral efficacy and a synergic effect respect to separate drugs, the heterodinucleotide 3TCpPMPA was synthesized. A single administration of the dimer as free drug or 3TCpPMPA-loaded RBC selectively targeted to M/M was able to almost completely protect macrophages from "de novo" infection.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenine / administration & dosage
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Adenine / analogs & derivatives*
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Adenine / chemical synthesis
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Adenine / chemistry
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Anti-HIV Agents / administration & dosage*
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / chemistry
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Drug Delivery Systems
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Drug Design
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Erythrocytes / metabolism
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HIV-1 / drug effects
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HIV-1 / physiology
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Humans
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In Vitro Techniques
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Lamivudine / administration & dosage
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Lamivudine / analogs & derivatives*
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Lamivudine / chemical synthesis
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Lamivudine / chemistry
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Macrophages / drug effects
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Macrophages / virology
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Organophosphonates / administration & dosage*
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Organophosphonates / chemical synthesis
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Organophosphonates / chemistry
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Tenofovir
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Virus Replication / drug effects
Substances
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Anti-HIV Agents
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Organophosphonates
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Lamivudine
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Tenofovir
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Adenine