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用于阴道萎缩的染料木黄酮包封的BDDE交联壳聚糖-TGA水凝胶的合成、表征及评价

Synthesis, characterization, and evaluation of BDDE crosslinked chitosan-TGA hydrogel encapsulated with genistein for vaginal atrophy.

作者信息

Yang I-Hsuan, Lin I-En, Chen Tzu-Chien, Chen Zhi-Yu, Kuan Che-Yung, Lin Jhih-Ni, Chou Yu-Chia, Lin Feng-Huei

机构信息

Department of Biomedical Engineering, College of Medicine and College of Engineering, National Taiwan University, No. 49, Fanglan Rd, Taipei, 10672, Taiwan.

Department of Biomedical Engineering, College of Medicine and College of Engineering, National Taiwan University, No. 49, Fanglan Rd, Taipei, 10672, Taiwan; Institute of Biomedical Engineering and Nanomedicine, National Health Research Institutes, No. 35, Keyan Road, Zhunan, Miaoli County, 35053, Taiwan.

出版信息

Carbohydr Polym. 2021 May 15;260:117832. doi: 10.1016/j.carbpol.2021.117832. Epub 2021 Feb 20.

Abstract

Vagina atrophy is a common symptom in women after menopause owing to decreasing estrogen levels. The most conventional treatment for this condition is estrogen cream. The shortcoming is its weak adhesion to the vagina mucus, thus requiring frequent daily application. In this study, BDDE was selected to crosslink and graft chitosan with thioglycolic acid, to form thiolated chitosan (CT) and improve the mucoadhesive properties of chitosan. Genistein was selected as the bioactive molecule that could exhibit estrogen-like properties for long-term treatment of vaginal atrophy. The efficacies of the materials were characterized and evaluated both in vitro and in vivo. Results showed that the mucoadhesive property of CT was approximately two-fold stronger against the constant flow than unmodified chitosan. CT with genistein (CT-G) was administered intravaginally every three days in vivo. It showed that the developed CT-G recover 54 % of the epithelium thickness of an atrophic vagina and ease vaginal atrophy.

摘要

阴道萎缩是绝经后女性的常见症状,原因是雌激素水平下降。针对这种情况,最传统的治疗方法是使用雌激素乳膏。其缺点是对阴道黏液的附着力较弱,因此需要每天频繁涂抹。在本研究中,选择1,4-丁二醇二缩水甘油醚将壳聚糖与巯基乙酸交联并接枝,形成硫醇化壳聚糖(CT),以改善壳聚糖的黏膜黏附特性。选择染料木黄酮作为具有雌激素样特性的生物活性分子,用于长期治疗阴道萎缩。对这些材料的功效进行了体外和体内表征及评估。结果表明,在恒定流动条件下,CT的黏膜黏附性能比未改性的壳聚糖强约两倍。在体内,含染料木黄酮的CT(CT-G)每三天经阴道给药一次。结果显示,所研发的CT-G可使萎缩阴道的上皮厚度恢复54%,并缓解阴道萎缩。

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