Inhibition of HIV-1 Replication in Macrophages by Red Blood Cell-Mediated Delivery of a Heterodinucleotide of Lamivudine and Tenofovir

P. Franchetti Department of Chemical Sciences, University of Camerino, Camerino, Italy

L. Cappellacci Department of Chemical Sciences, University of Camerino, Camerino, Italy

R. Petrelli Department of Chemical Sciences, University of Camerino, Camerino, Italy

P. Vita Department of Chemical Sciences, University of Camerino, Camerino, Italy

M. Grifantini Department of Chemical Sciences, University of Camerino, Camerino, Italy

L. Rossi Institute of Biochemistry “G. Fornaini,”, University of Urbino, Urbino, Italy

F. Pierigé Institute of Biochemistry “G. Fornaini,”, University of Urbino, Urbino, Italy

S. Serafini Institute of Biochemistry “G. Fornaini,”, University of Urbino, Urbino, Italy

M. Magnani Institute of Biochemistry “G. Fornaini,”, University of Urbino, Urbino, Italy

E. Balestra Department of Experimental Medicine, University of Rome “Tor Vergata,”, Rome, Italy

C.-F. Perno Department of Experimental Medicine, University of Rome “Tor Vergata,”, Rome, Italy

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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.

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Acknowledgments

This work was supported by grants from AIDS Project of the Italian National Institute of Health and by FIRB funds. (Red blood cells as drug carriers, RBNE01TBTR.)

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Inhibition of HIV-1 Replication in Macrophages by Red Blood Cell-Mediated Delivery of a Heterodinucleotide of Lamivudine and Tenofovir

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Inhibition of HIV-1 Replication in Macrophages by Red Blood Cell-Mediated Delivery of a Heterodinucleotide of Lamivudine and Tenofovir

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