Department of Physical Chemistry and Materials Science, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Műegyetem rkp. 3., H-1111 Budapest, Hungary.
Department of Physical Chemistry and Materials Science, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Műegyetem rkp. 3., H-1111 Budapest, Hungary.
Colloids Surf B Biointerfaces. 2022 May;213:112406. doi: 10.1016/j.colsurfb.2022.112406. Epub 2022 Feb 10.
Mucoadhesion testing at macroscopic scale needs a robust, convenient in vitro method as ex vivo methods suffer from poor reproducibility and ethical problems. Here we synthesized mucin-free poly(vinyl alcohol) (PVA) and mucin-containing PVA hydrogel substrates (Muc/PVA) to measure adhesion of polymer tablets. Freezing-thawing method was used for gelation to avoid chemical cross-linking and to preserve the functionality of mucin. The adhesion of first generation mucoadhesive polymers, poly(acrylic acid) (PAA) and hydroxypropylmethylcellulose (HPMC) was tested with outstanding reproducibility on individual batches of hydrogels and qualitative agreement with ex vivo literature data. Negatively charged PAA was less adhesive on Muc/PVA surface than on mucin-free PVA whereas HPMC as a neutral polymer displayed similar adhesion strength on both surfaces. Chitosan as a positively charged polymer showed enhanced adhesion on Muc/PVA substrate compared to mucin-free PVA. These results are corroborated by turbidimetric titration which indicated attractive electrostatic interactions between chitosan and mucin in contrast to the lack of attractive interactions for PAA and HPMC. These results prove the role of electronic theory in macroscopic mucoadhesion.
宏观尺度的黏膜黏附性测试需要一种稳健、便捷的体外方法，因为离体方法存在重复性差和伦理问题。在这里，我们合成了不含黏蛋白的聚乙烯醇（PVA）和含黏蛋白的聚乙烯醇水凝胶基质（Muc/PVA），以测量聚合物片剂的黏附性。采用冻融法使水凝胶发生胶凝，以避免化学交联并保持黏蛋白的功能。第一代黏膜黏附聚合物，聚丙烯酸（PAA）和羟丙基甲基纤维素（HPMC）的黏附性在各个批次的水凝胶上均具有出色的重现性，与离体文献数据具有定性一致性。带负电荷的 PAA 在不含黏蛋白的 PVA 表面上的黏附性低于 Muc/PVA 表面，而作为中性聚合物的 HPMC 在这两种表面上显示出相似的黏附强度。带正电荷的壳聚糖在 Muc/PVA 基质上的黏附性强于不含黏蛋白的 PVA。这些结果通过比浊滴定得到证实，比浊滴定表明壳聚糖和黏蛋白之间存在有吸引力的静电相互作用，而 PAA 和 HPMC 之间缺乏这种相互作用。这些结果证明了电子理论在宏观黏膜黏附性中的作用。
