Pharmacokinetics of UC781-loaded intravaginal ring segments in rabbits: a comparison of polymer matrices

Drug Delivery and Translational Research
Meredith R ClarkDavid R Friend

Abstract

UC781 is a potent and poorly water-soluble nonnucleoside reverse transcriptase inhibitor being investigated as a potential microbicide for preventing sexual transmission of HIV-1. This study was designed to evaluate the in vivo release and pharmacokinetics of UC781 delivered from matrix-type intravaginal ring segments in rabbits. Three polymer matrices (polyurethane, ethylene vinyl acetate copolymer, and silicone elastomer) and two drug loadings (5 and 15 mg/segment) were evaluated in at least one of two independent studies for up to 28 days in vivo. Inter-study comparison of in vivo release, vaginal tissue, and plasma concentrations for similar formulations demonstrated good reproducibility of the animal model. Mean estimates for a 28-day in vivo release ranged from 0.35 to 3.17 mg UC781 per segment. Mean proximal vaginal tissue levels (adjacent to the IVR segment) were 8-410 ng/g and did not change significantly with time for most formulations. Distal vaginal tissue levels of UC781 were 6- to 49-fold lower than proximal tissue levels. Mean UC781 plasma levels were low for all formulations, at 0.09-0.58 ng/mL. All formulations resulted in similar UC781 concentrations in vaginal tissue and plasma, except the low loading polyure...Continue Reading

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Apr 1, 2011·Drug Delivery and Translational Research·Meredith R ClarkDavid R Friend

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Citations

Apr 27, 2013·International Journal of Pharmaceutics·Justin M KeenRobert O Williams
May 3, 2014·Pharmaceutical Research·Ryan S TellerPatrick F Kiser
Oct 7, 2011·Journal of Pharmaceutical Sciences·Meredith R ClarkPatrick F Kiser
May 24, 2012·Journal of Pharmaceutical Sciences·Marc M BaumJohn A Moss
Feb 2, 2016·Advanced Drug Delivery Reviews·R Karl MalcolmDiarmaid J Murphy
Nov 30, 2011·Antimicrobial Agents and Chemotherapy·John A MossMarc M Baum

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