Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown, 2193, South Africa.
Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown, 2193, South Africa.
J Pharm Sci. 2023 Jun;112(6):1566-1585. doi: 10.1016/j.xphs.2023.02.021. Epub 2023 Mar 1.
Estrogens locally delivered to the vagina by tablets, capsules, rings, pessaries, and creams are the most common and highly recommended platforms to treat the genitourinary syndrome of menopause (GSM). Estradiol, an essential estrogen, is routinely administered alone, or in combination with progestins, to effectively alleviate the symptoms associated with moderate to severe menopause when non-pharmacological interventions are not indicated. Since the risk and side effects of estradiol use depends on the administered amount and duration of use, the lowest effective dose of estradiol is recommended when long-term treatment is required. Although there is a wealth of data and literature comparing vaginally administered estrogen-containing products, there is a lack of information revealing the effect of the delivery system used and formulation constituent's attributes on the efficacy, safety, and patient acceptability of these dosage forms. This review therefore aims to classify and compare various designs of commercially available and non-commercial vaginal 17β-estradiol formulations and analyze their performance in terms of systemic absorption, efficacy, safety, and patient satisfaction and acceptance. The vaginal estrogenic platforms included in this review are the currently marketed and investigational 17β-estradiol tablets, softgel capsules, creams, and rings for the treatment of GSM, based on their different design specifications, estradiol loads, and materials used in their preparation. Additionally, the mechanisms of the effects of estradiol on GSM have been discussed, as well as their potential impact on treatment efficacy and patient compliance.
雌激素可通过片剂、胶囊、环、栓剂和乳膏等局部递送至阴道，是治疗女性生殖泌尿系统绝经综合征（GSM）最常用和高度推荐的平台。雌二醇是一种必需的雌激素，通常单独使用或与孕激素联合使用，以有效缓解中度至重度绝经相关症状，当非药物干预不适用时。由于雌二醇使用的风险和副作用取决于给药量和使用时间长短，因此当需要长期治疗时，建议使用最低有效剂量的雌二醇。尽管有大量的数据和文献比较了阴道给予的含有雌激素的产品，但缺乏关于所使用的给药系统和制剂成分特性对这些剂型的疗效、安全性和患者可接受性的影响的信息。因此，本综述旨在对市售和非市售的 17β-雌二醇阴道制剂的各种设计进行分类和比较，并根据全身吸收、疗效、安全性以及患者满意度和接受度来分析它们的性能。本综述中纳入的阴道雌激素平台包括目前市售和正在研究的用于治疗 GSM 的 17β-雌二醇片剂、软胶囊、乳膏和环，基于它们不同的设计规格、雌二醇负荷和制备中使用的材料。此外，还讨论了雌二醇对 GSM 的作用机制，以及它们对治疗效果和患者依从性的潜在影响。
