Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center of RAS, 8 Arbuzov Str., 420088, Kazan, Russia; Kazan National Research Technological University, 68 Karl Marx Str., 420015, Kazan, Russia.
Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center of RAS, 8 Arbuzov Str., 420088, Kazan, Russia.
Colloids Surf B Biointerfaces. 2021 Dec;208:112089. doi: 10.1016/j.colsurfb.2021.112089. Epub 2021 Aug 31.
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.
黏液层作为一种选择性扩散屏障，对人体中药物传递系统的效率有重要影响。在这方面，目前正在广泛开发各种大小和组成的药物纳米载体，以研究它们的黏膜黏附特性，即与黏蛋白相互作用的能力。然而，由于在黏液层下的钙离子保留的上皮细胞形成了进一步的屏障，药物成分与黏蛋白的有效相互作用并不能保证成功。在这项工作中，首次考虑了黏蛋白（猪胃黏蛋白）与杯芳烃的相互作用。通过物理化学方法的复合物研究杯芳烃、黏蛋白和钙离子之间的相互作用表明，与黏蛋白的有效相互作用需要阳离子片段，并且由于杯芳烃结构中的阴离子片段而实现与钙的结合。因此，药物纳米载体结构中不同化学基团的结合在成功的黏膜药物传递中起着重要作用。考虑到大环平台的广泛合成修饰可能性，杯芳烃可以在穿过黏膜障碍的药物传递中找到应用。
