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基于点击化学的功能性海藻酸钠水凝胶的合成与评价及其在药物传递中的应用。

Synthesis and evaluation of functional alginate hydrogels based on click chemistry for drug delivery applications.

机构信息

BioTeam/ICPEES-ECPM, UMR CNRS 7515, Université de Strasbourg, Strasbourg Cedex 2, France.

BioTeam/ICPEES-ECPM, UMR CNRS 7515, Université de Strasbourg, Strasbourg Cedex 2, France.

出版信息

Carbohydr Polym. 2018 Jun 15;190:271-280. doi: 10.1016/j.carbpol.2018.02.086. Epub 2018 Mar 3.

DOI:10.1016/j.carbpol.2018.02.086
PMID:29628248
Abstract

Environment-sensitive alginate-based hydrogels for drug delivery applications are receiving increasing attention. However, most work in this field involves traditional cross-linking strategies which led to hydrogels with poor long-term stability. Herein, a series of chemically cross-linked alginate hydrogels was synthesized via click chemistry using Diels-Alder reaction by reacting furan-modified alginate and bifunctional cross-linkers. Alginate was successfully functionalized with furfurylamine. Then, 3D architectures were synthesized with water-soluble bismaleimides. Different substitution degrees were achieved in order to study the effect of alginate modification and the cross-linking extent over the behaviour of the hydrogels. The ensuing hydrogels were analysed in terms of microstructure, swelling, structure modification and rheological behaviour. The materials response to external stimuli such as pH was also investigated, revealing a pulsatile behaviour in a large pH range (1-13) and a clear pH-dependent swelling. Finally, vanillin release studies were conducted to demonstrate the potential of these biobased materials for drug delivery applications.

摘要

用于药物输送应用的环境敏感的基于海藻酸盐的水凝胶受到越来越多的关注。然而,该领域的大多数工作都涉及传统的交联策略,导致水凝胶的长期稳定性较差。在此,通过使用 Diels-Alder 反应通过呋喃修饰的海藻酸盐和双官能交联剂反应,通过点击化学合成了一系列化学交联的海藻酸盐水凝胶。海藻酸盐成功地用糠胺官能化。然后,用水溶性双马来酰亚胺合成了 3D 结构。为了研究海藻酸盐修饰和交联程度对水凝胶行为的影响,实现了不同的取代度。对所得水凝胶进行了微观结构、溶胀、结构修饰和流变行为的分析。还研究了材料对外界刺激(如 pH 值)的响应,结果表明在较大的 pH 值范围内(1-13)具有脉动行为和明显的 pH 值依赖性溶胀。最后,进行了香草醛释放研究,以证明这些基于生物的材料在药物输送应用中的潜力。

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