Oral administration of drugs is a two-edged sword – on one hand it is a non-invasive and easy-to-handle administration of drugs, on the other hand macromolecular pharmaceutical compounds cannot easily cross the epithelial barrier to reach systemic circulation or they could be inactivated in the gastrointestinal tract. Due the latter's nature with pH variations and proteolytic enzymes which digest and degrade external compounds, in particular peptides and proteins, oral delivery of macromolecular substances is an ongoing challenge in the field of pharmaceutical research. Several avenues of overcoming these drawbacks have been evaluated in the past, among them the promising approach of conjugation to natural and synthetic polymers. Polymers provide protection under harsh gastrointestinal conditions, may further enhance macromolecular drug absorption and pharmacological activity, and thus augment therapeutic efficiency. This short review highlights state-of-the-art developments in the field of oral macromolecule delivery and the benefit of polymer conjugation. We focus on a main review period from 2012 to 2017, and critically discuss latest developments for macromolecule engineering.

口服药物是一把两刃剑–一方面，它是无创且易于操作的药物管理，另一方面，大分子药物化合物无法轻易穿越上皮屏障达到全身循环，或者它们可以在胃肠道被灭活。由于后者的性质具有pH值变化和蛋白水解酶的作用，这些酶可以消化和降解外部化合物（特别是肽和蛋白质），因此大分子物质的口服给药一直是药物研究领域中的一个挑战。过去已经评估了克服这些缺点的几种途径，其中有希望的与天然和合成聚合物结合的方法。聚合物可在恶劣的胃肠道条件下提供保护，可以进一步增强大分子药物的吸收和药理活性，从而提高治疗效率。这篇简短的评论重点介绍了口服大分子递送领域的最新发展以及聚合物结合的优势。我们专注于2012年至2017年的主要审查期，并严格讨论高分子工程的最新发展。