Takacs Peter, Kozma Barbara, Rátonyi Dávid, Kozma Bence, Attila Kiss-Szikszai, Fenyvesi Ferenc, Sipos Attila G
Division of Female Pelvic Medicine and Reconstructive Surgery, Department of Obstetrics and Gynecology, Eastern Virginia Medical School, 825 Fairfax Avenue, Suite 526, Norfolk, VA 23507-2007, USA.
Department of Obstetrics and Gynecology, Faculty of Medicine, University of Debrecen, Nagyerdei krt. 98, 4032 Debrecen, Hungary.
Gels. 2024 Dec 13;10(12):823. doi: 10.3390/gels10120823.
Genitourinary syndrome of menopause (GSM) affects a significant percentage of postmenopausal women and manifests as vaginal dryness, irritation, and urinary discomfort, typically treated with vaginal estrogens. Hydrogels are preferred over creams due to their superior comfort and mucoadhesive properties. This study introduces a novel vaginal gel formulation containing hydroxyethyl cellulose (HEC) and estriol-hydroxypropyl-β-cyclodextrin complex (E3-HPBCD) for the treatment of GSM. The estriol (E3) release profile of the gel was evaluated using a Franz diffusion cell system, and its permeability was tested on reconstructed human vaginal epithelium. Biocompatibility was assessed using (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) (MTT), lactate dehydrogenase (LDH) assays, and real-time cell analysis (RTCA) on human skin keratinocyte (HaCaT) cells, which showed increased cell viability and no obvious cytotoxicity. The results indicated that efficient E3 release and satisfactory epithelial permeability with HPBCD provide the bioavailability of E3. These results suggest the potential of the gel as a biocompatible and effective alternative for the treatment of GSM. Further studies are required to assess the long-term safety and clinical efficacy.
更年期泌尿生殖综合征（GSM）影响着相当比例的绝经后女性，表现为阴道干燥、刺激和泌尿不适，通常采用阴道雌激素进行治疗。水凝胶因其卓越的舒适度和粘膜粘附特性而比乳膏更受青睐。本研究引入了一种新型阴道凝胶制剂，其含有羟乙基纤维素（HEC）和雌三醇 - 羟丙基 -β-环糊精复合物（E3-HPBCD），用于治疗GSM。使用Franz扩散池系统评估了该凝胶的雌三醇（E3）释放曲线，并在重建的人阴道上皮上测试了其渗透性。使用（3-[4,5-二甲基噻唑-2-基]-2,5-二苯基四氮唑溴盐）（MTT）、乳酸脱氢酶（LDH）测定法以及对人皮肤角质形成细胞（HaCaT）进行实时细胞分析（RTCA）来评估生物相容性，结果显示细胞活力增加且无明显细胞毒性。结果表明，E3与HPBCD一起实现了高效释放和令人满意的上皮渗透性，从而提供了E3的生物利用度。这些结果表明该凝胶作为治疗GSM的生物相容性和有效替代品具有潜力。需要进一步研究来评估其长期安全性和临床疗效。
