Ethylene vinyl acetate intravaginal rings for the simultaneous delivery of the antiretroviral UC781 and contraceptive levonorgestrel

Drug Delivery and Translational Research
Andrew LoxleyDavid R Friend

Abstract

Ethylene vinyl acetate intravaginal rings (IVRs) were prepared by hot-melt compounding and injection moulding. The IVRs contained various levels of the antiretroviral drug UC781 and the contraceptive hormone levonorgestrel. The IVRs were assayed for drug content and related substances, characterized for physical properties, in vitro drug-elution kinetics, photostress stability, and 3-month accelerated storage stability under ICH conditions. UC781 degrades on exposure to light and during thermal processing. UC22 is the major degradant of UC781. Drug release rates were proportional to drug loading, independent of the other drug in combination with IVRs, and were stable for 3 M at 40°C/75% RH despite changes in the appearance of the IVRs which is tentatively ascribed to crystallization of UC781 at or near the surface of the IVRs. The behavior of UC781 poses a substantial barrier to the commercial development of these IVRs.

References

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Citations

Aug 17, 2014·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Peter BoydChristopher McConville
Dec 1, 2012·Drug Delivery and Translational Research·Christopher McConvilleR Karl Malcolm
May 24, 2012·Journal of Pharmaceutical Sciences·Marc M BaumJohn A Moss
Feb 2, 2016·Advanced Drug Delivery Reviews·R Karl MalcolmDiarmaid J Murphy
Jun 21, 2015·Journal of Controlled Release : Official Journal of the Controlled Release Society·Shweta R UgaonkarThomas M Zydowsky
Feb 11, 2015·Drug Discovery Today·Milica StankovićWouter L J Hinrichs
May 23, 2015·Therapeutic Delivery·Christopher McConville
Dec 17, 2014·The Journal of Pharmacy and Pharmacology·Clara S BaffoeChristopher McConville
Oct 24, 2018·Journal of Materials Science. Materials in Medicine·Esmat Jalalvandi, Amin Shavandi
Dec 17, 2020·Polymers·Ioannis KoutsamanisEva Roblegg
Jun 3, 2021·Pharmaceutics·Louise CarsonRobert Karl Malcolm

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