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温敏水凝胶:一种适用于阴道给药的多功能概念。

Thermosensitive hydrogels a versatile concept adapted to vaginal drug delivery.

机构信息

a Department of Obstetrics and Gynecology, Division of Gynecologic Oncology , University of Utah Health Sciences , Salt Lake City , UT , USA.

b Department of Pharmaceutics and Pharmaceutical Chemistry , University of Utah , Salt Lake City , UT , USA.

出版信息

J Drug Target. 2018 Aug;26(7):533-550. doi: 10.1080/1061186X.2017.1400551. Epub 2017 Nov 15.

Abstract

Vaginal drug delivery represents an attractive strategy for local and systemic delivery of drugs otherwise poorly absorbed after oral administration. The rather dense vascular network, mucus permeability and the physiological phenomenon of the uterine first-pass effect can all be exploited for therapeutic benefit. However, several physiological factors such as an acidic pH, constant secretion, and turnover of mucus as well as varying thickness of the vaginal epithelium can impact sustained drug delivery. In recent years, polymers have been designed to tackle challenges mentioned above. In particular, thermosensitive hydrogels hold great promise due to their stability, biocompatibility, adhesion properties and adjustable drug release kinetics. Here, we discuss the physiological and anatomical uniqueness of the vaginal environment and how it impacts the safe and efficient vaginal delivery and also reviewed several thermosensitive hydrogels deemed suitable for vaginal drug delivery by addressing specific characteristics, which are essential to engage the vaginal environment successfully.

摘要

阴道给药代表了一种有吸引力的策略,可用于局部和全身递送口服后吸收不良的药物。相当密集的血管网络、黏液通透性以及子宫首过效应的生理现象都可以被利用来获得治疗益处。然而,一些生理因素,如酸性 pH 值、持续分泌和黏液的更新以及阴道上皮的厚度变化,都会影响药物的持续释放。近年来,人们设计了聚合物来解决上述挑战。特别是,温敏水凝胶因其稳定性、生物相容性、粘附性能和可调节的药物释放动力学而具有广阔的应用前景。在这里,我们讨论了阴道环境的生理和解剖学独特性,以及它如何影响安全有效的阴道给药,并综述了几种被认为适合阴道药物递送的温敏水凝胶,通过解决与成功结合阴道环境相关的特定特征来实现这一目标。

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