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02662 POTENTIAL REMEDYS FOR DELIVERY OF HIGH-EFFECTIVE MEMBRANE-ACTING ANTI-HIV MICROBICIDES data not supplied Annually several million persons get infected with HIV via sexual route. To protect those who do not use contraceptives, efficient preparations are necessary: microbicids of vaginal application. As a rule, preparations exhibiting efficient anti-HIV action in vitro cause irritation when applied locally on vaginal mucous membrane, which can cause a decrease in antiviral activity, perhaps due to involvement of ?D4+ cells. In the present work, we investigated routes for the creation of efficient pharmaceutical form of microbicid preparation based on conjugates of polymeric carboxylic acid with adamantane, norbornane, norbornene, and peptide imitators of HIV-1/2 coreceptors. In order to eliminate irritating action and increase microbicid activity, we included efficient membrane-acting anti-HIV compounds into the ??-dependent interpolymeric complex (IPC) which is stable into weakly acidic media and decomposes with the release of active anti-HIV preparation in neutral and/or alkaline media, with one of the following polymers: sodium alginate, polyvinylpyrrolidone (PVP), partly hydrolyzed chitosan, polyvinylimidazole, or included into the complex: PVP-polyacrylic acid. We propose to use carbopole, hyaluronic acid, sodium alginate, or chitosan (depending on the IPC used) as a gel-forming component for the final pharmaceutical form. The anti-HIV efficiency of some IPC proposed has been demonstrated experimentally in vitro, along with a decrease in local toxic action of preparation included in the IPC in vivo when applied on Dr Tatyana Ryabicheva |
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