Development of a UC781 releasing poly ethylene vinyl acetate vaginal ring

Christopher McConville, Ian Major, Meredith R. Clark, R. Karl Malcolm

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)489-497
Number of pages11
JournalDrug Delivery and Translational Research
Volume2
DOIs
Publication statusPublished - 07 Sept 2012

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