A novel anastrozole intravaginal ring for endometriosis: Pharmacokinetic characteristics and mucosal irritation
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An anastrozole intravaginal ring made of EVA was evaluated in mini pigs, showing comparable pharmacokinetics to oral tablets, passive uterine targeting, and acceptable mucosal irritation.
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Abstract
In order to achieve the long-term management of endometriosis, a more economical and environmentally friendly material, ethylene vinyl acetate (EVA), was used to prepare a intravaginal ring with anastrozole (ATZ). This paper has compared the pharmacokinetic parameters with oral tablets (Aida®) in mini pigs and evaluated the uterine targeted effect and mucosal irritation of the ring. A bioassay method was developed and validated for the determination of ATZ in mini pigs. The determination of ATZ was achieved by LC-MS/MS using terfenadine as the internal standard. Separation was achieved on a Kinetex-C18 110A chromatographic column (3 × 30 mm, 2.6 μm; Phenomenex) with a gradient mobile phase consisting of methanol (0.1% formic acid) and water (0.1% formic acid). The method has been proved to be scientific and sensitive through methodological validation and can be easily and quickly applied to the determination of the content of anastrozole in mini pigs. The pharmacokinetic test results show that there was no significant difference in pharmacokinetic parameters between the two formulations. The intravaginal ring has a passive targeting effect on the uterus, and its mucosal irritation is acceptable. The intravaginal ring provides a new method for long-term management of endometriosis.
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Cites (4)
- Anastrazole and oral contraceptives: a novel treatment for endometriosis 2005
- Estrogen biosynthesis in endometriosis: molecular basis and clinical relevance 2000
- Characterization of anastrozole effects, delivered by an intravaginal ring in cynomolgus monkeys 2014
- Preparation and <i>in vitro/in vivo</i> evaluation of anastrozole reservoir‐type intravaginal ring 2018
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Source provenance
- europepmc
- last seen: 2026-06-17T06:13:18.893374+00:00
- openalex
- last seen: 2026-06-10T17:14:06.276822+00:00
- pubmed
- last seen: 2026-06-17T06:12:28.819509+00:00
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