title: Liposomal encapsulation enhances antiviral efficacy of SPC3 against human immunodeficiency virus type-1 infection in human lymphocytes.
abstract: Because encapsulation of antiviral drugs in liposomes resulted generally in improved activity against retroviral replication in vivo, the antiviral effects of free-SPC3 and liposome-associated SPC3 were compared in cultured human lymphocytes infected with HIV-1. SPC3 was entrapped in various liposomal formulations, either different in size (mean diameter of 100 and 250 nm), SPC3 concentration or cholesterol content. Liposome-associated SPC3 were tested for both inhibition of cell-cell fusion and infection with HIV-1 clones. SPC3 inhibited HIV-1-induced fusion at a micromolar concentration range. When associated with liposomes, SPC3 was found to be about 10-fold more potent than free SPC3 in inhibiting syncytium formation. Continuous treatment with free SPC3 also inhibited virus production in a dose-dependent manner, with inhibition of HIV infection of C8166 T-cells or human peripheral blood lymphocytes (PBLs) at micromolar concentrations. Liposomal entrapment was found to increase the antiviral efficacy of SPC3 by more than 10- and 5-fold in C8166 and PBLs, respectively. These data suggest that the liposome approach may be used to improve SPC3 antiviral efficacy.
authors.affiliation: CNRS UMR 6560, Laboratoire de Biochimie, Ingéniérie des Protéines, Faculté de Médecine Secteur Nord, 13916 Marseille Cedex 20, France.
authors.forename: Jean
authors.initials: J
authors.lastname: de Mareuil
authors.forename: Kamel
authors.initials: K
authors.lastname: Mabrouk
authors.forename: Evelyne
authors.initials: E
authors.lastname: Doria
authors.forename: Maxime
authors.initials: M
authors.lastname: Moulard
authors.forename: Stéphanie
authors.initials: S
authors.lastname: de Chasteigner
authors.forename: Razika
authors.initials: R
authors.lastname: Oughideni
authors.forename: Jurphaas
authors.initials: J
authors.lastname: van Rietschoten
authors.forename: Hervé
authors.initials: H
authors.lastname: Rochat
authors.forename: Michel
authors.initials: M
authors.lastname: De Waard
authors.forename: Jean-Marc
authors.initials: JM
authors.lastname: Sabatier
mesh_terms: D000998:Antiviral Agents / Q000008:administration & dosage*; D002784:Cholesterol / Q000008:administration & dosage / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D015726:Giant Cells / Q000187:drug effects; D015699:HIV Envelope Protein gp120 / Q000008:administration & dosage*; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D008081:Liposomes; D008214:Lymphocytes / Q000821:virology*; D011994:Recombinant Proteins
chemical_list: D000998:Antiviral Agents; D015699:HIV Envelope Protein gp120; D008081:Liposomes; D011994:Recombinant Proteins; C098257:SPC3 peptide; D002784:Cholesterol