A Dual Stimuli Responsive Supramolecular Gel Provides Insulin Hydrolysis Protection and Redox‐Controlled Release of Actives,Macromolecular Chemistry and Physics

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A Dual Stimuli Responsive Supramolecular Gel Provides Insulin Hydrolysis Protection and Redox‐Controlled Release of Actives
Macromolecular Chemistry and Physics ( IF 2.5 ) Pub Date : 2020-01-13 , DOI: 10.1002/macp.201900419
Diego Navarro‐Barreda ₁ , César A. Angulo‐Pachón ₁ , Begoña Bedrina ₁ , Francisco Galindo ₁ , Juan F. Miravet ₁

Affiliation

Two supramolecular hydrogelators containing a central disulfide moiety and terminal carboxylic acid groups are studied. On the one hand, the hydrogels are responsive to a reductive environment, which transforms the disulfide unit to the corresponding thiols. On the other hand, the hydrogels show pH response associated with the presence of carboxylic acid units. Gels are formed at pH below ≈4 while at higher pH values, ionization of the gelators provokes gel disassembly. The properties of the gel are exploited for the release, as a proof of concept, of Bromophenol Blue in the presence of the reducing species tris(2‐carboxyethyl)phosphine hydrochloride. Additionally, insulin is loaded into the hydrogels and protected from hydrolysis with simulated gastric fluid containing pepsin. Quantitative release of unaltered insulin, checked with an enzyme‐linked immunosorbent assay colorimetric assay, is observed upon treatment with pH 7.4 buffer. This behavior would permit the use of the new hydrogels for oral insulin delivery.

中文翻译：

双重刺激响应性超分子凝胶可提供胰岛素水解保护和活性物质的氧化还原控制释放

研究了两个包含中心二硫键部分和末端羧酸基团的超分子水凝胶剂。一方面，水凝胶对还原环境有反应，该还原环境将二硫键单元转化为相应的硫醇。另一方面，水凝胶显示出与羧酸单元的存在有关的pH响应。在低于≈4的pH值下会形成凝胶，而在更高的pH值下，胶凝剂的电离会引起凝胶分解。作为概念的证明，利用凝胶的特性在还原性三（2-羧乙基）膦盐酸盐存在下释放溴酚蓝。另外，将胰岛素加载到水凝胶中，并用含有胃蛋白酶的模拟胃液保护其免受水解。定量释放未改变的胰岛素，用pH 7.4缓冲液处理后，观察到用酶联免疫吸附比色法检查的结果。这种行为将允许使用新的水凝胶口服胰岛素递送。

更新日期：2020-01-13

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