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用于口服给药的具有双重响应性的氨基酸基水凝胶。

Amino Acid Based Hydrogels with Dual Responsiveness for Oral Drug Delivery.

作者信息

Wang Shiqi, Liu Xiaoxue, Villar-Garcia Ignacio J, Chen Rongjun

机构信息

Department of Chemical Engineering, Imperial College London, South Kensington Campus, London, SW7 2AZ, UK.

Department of Materials, Imperial College London, South Kensington Campus, London, SW7 2AZ, UK.

出版信息

Macromol Biosci. 2016 Sep;16(9):1258-64. doi: 10.1002/mabi.201600078. Epub 2016 May 6.

Abstract

This study reports a series of novel amino acid based dual-responsive hydrogels. Prepared by a facile one-pot 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) coupling reaction, the solid content, structure, and mechanical behavior of hydrogels could be easily adjusted by changing the concentrations of the polymers and the crosslinkers. With pH-responsive anionic pseudo-peptides as backbones and disulfide-containing l-cystine dimethyl ester as crosslinkers, these hydrogels are able to collapse and form relatively compact structure at an acidic pH, while swelled and partly dissociated at a neutral pH. Further addition of dithiothreitol (DTT) facilitated complete degradation of hydrogels. The high loading efficiency, rapid but complete triggered-release, and good biocompatibility make these hydrogels promising candidates for oral delivery.

摘要

本研究报道了一系列新型的基于氨基酸的双响应水凝胶。通过简便的一锅法1-乙基-3-(3-二甲基氨基丙基)碳二亚胺(EDC)偶联反应制备,通过改变聚合物和交联剂的浓度,可以轻松调节水凝胶的固含量、结构和力学行为。以pH响应性阴离子假肽为主链,含二硫键的L-胱氨酸二甲酯为交联剂,这些水凝胶在酸性pH值下能够塌陷并形成相对致密的结构,而在中性pH值下膨胀并部分解离。进一步添加二硫苏糖醇(DTT)促进了水凝胶的完全降解。高负载效率、快速但完全的触发释放以及良好的生物相容性使这些水凝胶成为口服给药的有前途的候选者。

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