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Thiolated polymers: Bioinspired polymers utilizing one of the most important bridging structures in nature

机译:硫醇化聚合物:生物悬浮的聚合物,利用自然界中最重要的桥接结构之一

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摘要

Thiolated polymers designated "thiomers" are obtained by covalent attachment of thiol functionalities on the polymeric backbone of polymers. In 1998 these polymers were first described as mucoadhesive and in situ gelling compounds forming disulfide bonds with cysteine-rich substructures of mucus glycoproteins and crosslinking through inter- and intrachain disulfide bond formation. In the following, it was shown that thiomers are able to form disulfides with keratins and membrane-associated proteins exhibiting also cysteine-rich substructures. Furthermore, permeation enhancing, enzyme inhibiting and efflux pump inhibiting properties were demonstrated. Because of these capabilities thiomers are promising tools for drug delivery guaranteeing a strongly prolonged residence time as well as sustained release on mucosal membranes. Apart from that, thiomers are used as drugs per se. In particular, for treatment of dry eye syndrome various thiolated polymers are in development and a first product has already reached the market. Within this review an overview about the thiomer-technology and its potential for different applications is provided discussing especially the outcome of studies in non-rodent animal models and that of numerous clinical trials. Moreover, an overview on product developments is given.
机译:通过在聚合物的聚合物主链上的硫醇官能团的共价附着来获得硫醇化聚合物。 1998年,这些聚合物首先被描述为粘膜粘附和原位胶凝化合物,形成二硫键,其与粘液糖蛋白的富含半胱氨酸的富含粘合剂的子结构和通过间交联通过间交联通过间相互依赖的二硫键形成。在下文中,表明巯基能够与角蛋白和膜相关蛋白形成二硫化物,也能表现出富含半胱氨酸的子结构的半胱氨酸。此外,证明了渗透增强,酶抑制和流出泵抑制性能。由于这些能力,巯基是有助于药物递送的工具,可保证强烈延长的停留时间以及粘膜上的持续释放。除此之外,巯基将用作药物本身。特别是,对于干眼症综合征的治疗,各种硫醇化聚合物正在开发中,并且已经达到了市场。在这篇文章中,提供了关于巯基技术及其对不同应用的潜力的概述,特别是讨论非啮齿动物模型的研究结果以及许多临床试验。此外,给出了产品开发的概述。

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