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载芹黄素的 pH 敏感型微乳填充胶凝多糖水凝胶:特性与体外释放动力学。

A pH-sensitive microemulsion-filled gellan gum hydrogel encapsulated apigenin: Characterization and in vitro release kinetics.

机构信息

College of Chemistry, Chemical Engineering and Materials Science, Shandong Normal University, Jinan 250014, PR China.

College of Chemistry, Chemical Engineering and Materials Science, Shandong Normal University, Jinan 250014, PR China.

出版信息

Colloids Surf B Biointerfaces. 2019 Jun 1;178:245-252. doi: 10.1016/j.colsurfb.2019.03.015. Epub 2019 Mar 7.

Abstract

In this work, the incorporation of O/W microemulsion in gellan gum hydrogels was performed to prepare the composite hydrogel as the carrier of apigenin. In vitro release studies resulted that the composite hydrogels could control the drug release under acidic (pH 1.2) and weak alkaline conditions (pH 7.4). This was due to the increase of crosslinking degree under acidic medium and degradation under weak alkaline medium, observed by SEM technique. The FT-IR analysis further confirmed that the hydrogen ions (H) under acidic conditions could diminish the electrostatic repulsion between the gellan gum molecules by offsetting the negative charge of carboxyl groups, promoting the formation of double helices. The in vitro release kinetics resulted that the release under acidic conditions was a Fickian diffusion-controlled mechanism. While the in vitro release under weak alkaline condition was erosion-controlled mechanism. In addition, the components of microemulsion have also an influence on the release behavior, which was related to the diameter distributions of microemulsion droplets and the hydrogen bond degrees between surfactants and polymers. As a result, the microemulsion-filled hydrogels could be a promising pH-controlled release system for oral delivery of hydrophobic drug.

摘要

在这项工作中,将 O/W 微乳液掺入到结冷胶水凝胶中,以制备用作芹菜素载体的复合水凝胶。体外释放研究表明,复合水凝胶可以在酸性(pH 1.2)和弱碱性条件(pH 7.4)下控制药物释放。这是由于在酸性介质中交联度增加以及在弱碱性介质中降解,通过 SEM 技术观察到。FT-IR 分析进一步证实,酸性条件下的氢离子(H)可以通过抵消羧基的负电荷来减少结冷胶分子之间的静电排斥,从而促进双螺旋的形成。体外释放动力学表明,酸性条件下的释放是菲克扩散控制机制。而在弱碱性条件下的体外释放则是侵蚀控制机制。此外,微乳液的成分也会影响释放行为,这与微乳液液滴的直径分布以及表面活性剂与聚合物之间的氢键程度有关。因此,填充有微乳液的水凝胶可能是一种有前途的 pH 控制释放系统,可用于口服递送疏水性药物。

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