Development of a UC781 releasing polyethylene vinyl acetate vaginal ring

Drug Delivery and Translational Research
Christopher McconvilleR Karl Malcolm

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.

References

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Citations

Jun 3, 2014·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Nhung T T DangAllan G A Coombes
Aug 17, 2014·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Peter BoydChristopher McConville
Feb 2, 2016·Advanced Drug Delivery Reviews·R Karl MalcolmDiarmaid J Murphy
May 23, 2015·Therapeutic Delivery·Christopher McConville
Dec 17, 2014·The Journal of Pharmacy and Pharmacology·Clara S BaffoeChristopher McConville
Jun 10, 2017·Drug Delivery and Translational Research·Ian Major, Christopher McConville
Jun 3, 2021·Pharmaceutics·Louise CarsonRobert Karl Malcolm
Jun 27, 2020·Current Pharmaceutical Design·Abimanyu Sugumaran, Vishali Mathialagan
Jul 20, 2021·Geburtshilfe und Frauenheilkunde·Fojan RafieiKhosrow Mottaghy

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