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. 2011 Apr;100(4):1416-35.
doi: 10.1002/jps.22365. Epub 2010 Oct 19.

In Vivo Evaluation of the Release of Zidovudine and Polystyrene Sulfonate From a Dual Intravaginal Bioadhesive Polymeric Device in the Pig Model

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In Vivo Evaluation of the Release of Zidovudine and Polystyrene Sulfonate From a Dual Intravaginal Bioadhesive Polymeric Device in the Pig Model

Valence M K Ndesendo et al. J Pharm Sci. .

Abstract

This study focused on determining the concentration of zidovudine (AZT) and polystyrene sulfonate (PSS) in the plasma and vaginal tissue of the large white pig from an intravaginal bioadhesive polymeric device (IBPD). Biocompatible polymers were compressed with AZT and PSS into caplet-shaped devices for insertion into the posterior fornix of the pig vagina. A total of 25 pigs were used in this study. Plasma was sampled from the jugular vein at various time points after insertion of the IBPD reaching 28 days. At day 28, the pigs were euthanized and vaginal tissue was removed and digested with subtilisin for AZT and PSS extraction. The mean concentration detected in vaginal tissue at day 28 was 1.214 ± 0.062 mg/mL for AZT and 1.400 ± 0.071 mg/mL for PSS. Plasma concentration was significantly lower for AZT (0.332 ± 0.014 mg/mL) and PSS (0.256 ± 0.013 mg/mL). This indicated higher retention of AZT and PSS within the vaginal tissue. Molecular mechanics simulations blueprinted polymer-drug-mucin force-field interactions and energies that explicated the spatial preference of AZT and PSS for the vaginal tissue. Histopathotoxicity studies revealed negative-to-mild foreign body events and results strongly suggest that the IBPD may be suitable for prolonged intravaginal drug delivery in preventing the transmission of sexually transmitted infections and HIV/AIDS.

Keywords: HIV/AIDS; STIs; formulation; intravaginal drug delivery; molecular dynamics; permeability; large white pig model; pharmacokinetics; polymeric drug delivery systems; zidovudine; polystyrene sulfonate.

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