Interdisciplinary Nanoscience Center (iNANO), Aarhus University, Gustav-Wieds Vej 14, 8000, Aarhus, Denmark.
Macromol Biosci. 2017 Sep;17(9). doi: 10.1002/mabi.201700060. Epub 2017 Jul 4.
Although oral is the preferred route of administration of pharmaceutical formulations, the long-standing challenge for medically active compounds to efficiently cross the mucus layer barrier limits its wider applicability. Efforts in nanomedicine to overcome this hurdle consider mucoadhesive and mucopenetrating drug carriers by selectively designing (macromolecular) building blocks. This review highlights and critically discusses recent strategies developed in this context including poly(ethylene glycol)-based modifications, cationic and thiolated polymers, as well as particles with high charge density, zeta-potential shifting ability, or mucolytic properties. The latest advances in ex vivo test platforms are also reviewed.
虽然口服是药物制剂的首选给药途径,但对于具有医学活性的化合物来说,要有效地穿过黏液层屏障仍然是一个长期存在的挑战,这限制了其更广泛的应用。纳米医学领域的研究致力于通过有针对性地设计(高分子)构建块来克服这一障碍,例如使用黏附性和穿透黏液的药物载体。本文重点介绍并批判性地讨论了这方面的最新策略,包括基于聚乙二醇的修饰、阳离子和巯基聚合物,以及具有高电荷密度、zeta 电位转移能力或粘液溶解特性的颗粒。本文还回顾了最新的离体测试平台的进展。