Chitosan-catechol: A polymer with long-lasting mucoadhesive properties
Chitosan-catechol: A polymer with long-lasting mucoadhesive properties
复制标题
DOI：
10.1016/j.biomaterials.2015.02.010
复制
发表时间：
2015-06-01
期刊：
影响因子：
14
通讯作者：
Lee, Haeshin
中科院分区：
文献类型：
--
作者：
Kim, Kyuri;Kim, Keumyeon;Lee, Haeshin
许多粘膜粘附聚合物已被用于延长配制的药物或药物在特定递送部位的停留时间。然而，很难获得令人满意的粘膜粘附特性。硫醇化或凝集素功能化等两种主要的修饰策略已被广泛研究，但硫醇化情况下二硫键的可逆性和凝集素的毒性一直是问题。因此，需要开发进一步改善粘膜粘附特性的方法。拥有大量的粘膜粘附聚合物，改善粘膜粘附的一种实用方法是对现有的粘膜粘附聚合物进行化学修饰。换句话说，该方法基于利用协同效应，该协同效应可以通过将小的粘附部分化学束缚到可用的粘膜粘附聚合物来实现。在这里，我们将源自贻贝粘附蛋白的儿茶酚与壳聚糖结合，壳聚糖是一种众所周知的粘膜粘附聚合物。我们证明，与未修饰的壳聚糖相比，壳聚糖儿茶酚的胃肠道（GI）滞留得到改善，这是由于与粘蛋白形成了不可逆的儿茶酚介导的交联。结果表明，粘膜粘附聚合物的儿茶酚修饰可能会产生用于粘膜药物递送的新一代粘膜粘附聚合物。 (C) 2015 Elsevier Ltd. 保留所有权利。
Numerous mucoadhesive polymers have been exploited for prolonging the residence time of formulated drugs or pharmaceuticals at specific delivery sites. However, it has been difficult to achieve satisfactory mucoadhesive properties. The two major modification strategies such as thiolation or lectin functionalization have been extensively studied, but disulfide bond reversibility in the case of thiolation and the toxicity of lectins have been problems. Thus, approaches for further improvement of mucoadhesive properties need to be developed. With an overwhelming library of mucoadhesive polymers, one practical way to improve mucoadhesion is chemical modification of existing mucoadhesive polymers. In other words, the method is based on utilizing the cooperative effect that might be achieved by chemical tethering of a small adhesive moiety to an available mucoadhesive polymer. Here, we conjugated catechols derived from mussel adhesive proteins to chitosan, which is a widely known mucoadhesive polymer. We demonstrated that the gastrointestinal (GI) tract retention of chitosancatechol was improved compared to unmodified chitosan, which is due to the formation of irreversible catechol mediated-crosslinking with mucin. The results indicate that catechol modification of mucoadhesive polymers may possibly lead to a new generation of mucoadhesive polymers for mucosal drug delivery. (C) 2015 Elsevier Ltd. All rights reserved.