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Development of a UC781 releasing polyethylene vinyl acetate vaginal ring

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Abstract

UC781 is potent, hydrophobic, non-nucleotide reverse transcriptase inhibitor (NNRTI) against the human immunodeficiency virus (HIV). UC781 is currently being investigated for use as a potential HIV microbicide. A study in rhesus macaques demonstrated that a 100-mg UC781-loaded silicone elastomer vaginal ring released limited amounts of UC781 into the vaginal fluid and tissue after 28 days. The reason for this was due to the hydrophobic nature and limited aqueous solubility of UC781. This study describes the manufacture of UC781-loaded polyethylene vinyl acetate (PEVA) vaginal rings, which have an improved in vitro release rate of UC781 when compared to UC781-loaded silicone elastomer vaginal rings. The study demonstrates that the UC781 in the PEVA rings is mostly in its amorphous form due to the rings being manufactured above UC781’s melting point. Furthermore, the rings do not show any signs of UC781 degradation, such as the presence of UC22.

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Authors and Affiliations

  1. School of Pharmacy, Medical Biology Centre, Queen’s University of Belfast, 97 Lisburn Road, Belfast, BT9 7BL, Northern Ireland, UK

    Christopher McConville, Ian Major & R. Karl Malcolm

  2. CONRAD, 1911 North Fort Myer Drive, Suite 900, Arlington, VA, 22209, USA

    David R. Friend & Meredith R. Clark

  3. Department of Pharmacy, School of Applied Sciences, University of Wolverhampton, Wulfrana Street, Wolverhampton, WV1 1LY, UK

    Christopher McConville

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  1. Christopher McConville
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  2. Ian Major
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  3. David R. Friend
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  4. Meredith R. Clark
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  5. R. Karl Malcolm
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Correspondence to Christopher McConville.

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McConville, C., Major, I., Friend, D.R. et al. Development of a UC781 releasing polyethylene vinyl acetate vaginal ring. Drug Deliv. and Transl. Res. 2, 489–497 (2012). https://doi.org/10.1007/s13346-012-0101-3

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