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Interaction of mucin with viologen and acetate derivatives of calix[4]resorcinols
Colloids and Surfaces B: Biointerfaces ( IF 5.8 ) Pub Date : 2021-08-31 , DOI: 10.1016/j.colsurfb.2021.112089
Ruslan R Kashapov 1 , Nadezda E Kashapova 2 , Albina Y Ziganshina 2 , Victor V Syakaev 2 , Vitaliy V Khutoryanskiy 3 , Lucia Y Zakharova 1
Affiliation  

The mucus layer acts as a selective diffusion barrier that has an important effect on the efficiency of drug delivery systems in the human body. In this regard, currently the drug nanocarriers of various sizes and compositions are being widely developed to study their mucoadhesive properties i.e., the ability to interact with mucin. However, the effective interaction of drug composition with mucin does not guarantee the success due to the fact that there is a further barrier in the form of epithelial cells retained by calcium ions under the mucus layer. In this work, the interaction of mucin (porcine gastric mucin) with calixarenes is considered for the first time. The study of interaction between calixarenes, mucin and calcium ions by a complex of physicochemical methods showed that effective interaction with mucin requires cationic fragments, and binding with calcium is realized due to anionic fragments in the calixarene structure. Therefore, the combination of different chemical groups in the structure of drug nanocarrier plays an important role in successful mucosal drug delivery. Taking into account the wide possibilities of synthetic modification of the macrocyclic platform, calixarenes can find the application in the drug delivery across mucous barriers.



中文翻译:

粘蛋白与杯[4]间苯二酚的紫精和醋酸酯衍生物的相互作用

The mucus layer acts as a selective diffusion barrier that has an important effect on the efficiency of drug delivery systems in the human body. 在这方面,目前正在广泛开发各种尺寸和组成的药物纳米载体以研究它们的粘膜粘附特性​​,即与粘蛋白相互作用的能力。然而,药物组合物与粘蛋白的有效相互作用并不能保证成功,因为在粘液层下存在以钙离子保留的上皮细胞形式的进一步屏障。在这项工作中,首次考虑了粘蛋白(猪胃粘蛋白)与杯芳烃的相互作用。通过复合物化方法研究杯芳烃、粘蛋白和钙离子之间的相互作用表明,与粘蛋白的有效相互作用需要阳离子片段,由于杯芳烃结构中的阴离子片段,实现了与钙的结合。因此,药物纳米载体结构中不同化学基团的组合对于成功的粘膜药物递送具有重要作用。考虑到大环平台合成修饰的广泛可能性,杯芳烃可以在跨越粘膜屏障的药物递送中找到应用。

更新日期:2021-09-07
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