Use of simulated vaginal and menstrual fluids to model in vivo discolouration of silicone elastomer vaginal rings.

Autor: McCoy CF; School of Pharmacy, Queen's University Belfast, Belfast BT9 7BL, UK., Spence P; International Partnership for Microbicides, Silver Spring, MD 20910, USA., Dallal Bashi YH; School of Pharmacy, Queen's University Belfast, Belfast BT9 7BL, UK., Murphy DJ; School of Pharmacy, Queen's University Belfast, Belfast BT9 7BL, UK., Boyd P; School of Pharmacy, Queen's University Belfast, Belfast BT9 7BL, UK., Dangi B; International Partnership for Microbicides, Silver Spring, MD 20910, USA., Derrick T; International Partnership for Microbicides, Silver Spring, MD 20910, USA., Devlin B; International Partnership for Microbicides, Silver Spring, MD 20910, USA., Kleinbeck K; International Partnership for Microbicides, Silver Spring, MD 20910, USA., Malcolm RK; School of Pharmacy, Queen's University Belfast, Belfast BT9 7BL, UK.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics: X [Int J Pharm X] 2021 May 01; Vol. 3, pp. 100081. Date of Electronic Publication: 2021 May 01 (Print Publication: 2021).
DOI: 10.1016/j.ijpx.2021.100081
Abstrakt: Vaginal rings releasing antiretrovirals - either alone or in combination with contraceptive progestins - are being developed for prevention of human immunodeficiency virus (HIV) transmission via vaginal sex. Following Phase I trials, significant discolouration was observed on the surface of investigational silicone elastomer antiretroviral-contraceptive matrix-type vaginal rings containing either 25 mg dapivirine or 200 mg dapivirine plus levonorgestrel. In this study, potential causes of the discolouration have been assessed in vitro using simulated vaginal and menstrual fluids (SVF and SMF, respectively) to model in vivo exposure. The fluid compositions also included hydrogen peroxide (H 2 O 2 ), hydrogen peroxide plus a copper intrauterine device (IUD), or synthetic dyes (representing personal care and household cleaning products). No discolouration was observed for rings exposed to SVF + hydrogen peroxide (with or without an IUD). However, the SVF + dye compositions showed significant ring discolouration, with staining patterns similar to those observed with rings that had been exposed to highly-coloured personal care and household cleaning products during clinical trial use. Exposure of rings to SMF compositions invariably caused yellow surface discolouration, dark spotting and markings, similar to the staining patterns observed following clinical use. The darker marks on the ring surface were identified as blood debris derived from the SMF. The study indicates that surface discolouration of rings in vivo can be attributed to exposure to menstrual fluid or highly coloured personal care or household cleaning products. Discolouration of the rings was not associated with any specific safety risks for the user, though severe discolouration could potentially impact acceptability and adherence.
Competing Interests: All authors declare no actual or potential conflicts of interest.
(© 2021 The Author(s).)
Databáze: MEDLINE
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