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• W1869745831 abstract "<h2>ABSTRACT</h2> Tenofovir was incorporated in controlled-release polycaprolactone (PCL) matrices designed for production of vaginal inserts for prevention of HIV transmission. Rapid cooling of suspensions of the drug powder in PCL solution resulted in micro-porous matrices with tenofovir loadings up to 12% (w/w) and high incorporation efficiencies in excess of 90%. The release behaviour of tenofovir in simulated vaginal fluid (SVF) demonstrated high delivery efficiency of 85%–99% over 30 days and could be described effectively by a first-order kinetics model giving a mean value of 0.126 day-1 for the release constant (<i>k</i>₁). Tenofovir released from PCL matrices into SVF exhibited high relative activity ranging from 70 to 90%, against pseudo-typed HIV-1-infected HeLa cells. The inhibitory activity of tenofovir standard solutions in SVF provided an IC₅₀ value of 2.38μM. Besides confirming high levels of <i>in vitro</i> antiviral activity, the predicted concentrations of tenofovir, which would be released from a PCL intra-vaginal ring <i>in vivo</i>, exceeded the IC50 value for HIV-1 by a factor of 35–200 and clinically protective concentrations by a factor of 50. These findings recommend further investigations of antiviral-loaded PCL matrices for controlling heterosexual transmission of HIV." @default.
• W1869745831 created "2016-06-24" @default.
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• W1869745831 date "2013-10-01" @default.
• W1869745831 modified "2023-09-24" @default.
• W1869745831 title "An Evaluation of Polycaprolactone Matrices for Vaginal Delivery of the Antiviral, Tenofovir, in Preventing Heterosexual Transmission of HIV" @default.
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• W1869745831 doi "https://doi.org/10.1002/jps.23684" @default.
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