Department of Chemistry, Aarhus University, Aarhus C 8000, Denmark.
iNano Interdisciplinary Nanoscience Centre, Aarhus University, Aarhus C 8000, Denmark.
Nat Chem. 2016 Oct 21;8(11):997-1007. doi: 10.1038/nchem.2629.
Biological drugs generated via recombinant techniques are uniquely positioned due to their high potency and high selectivity of action. The major drawback of this class of therapeutics, however, is their poor stability upon oral administration and during subsequent circulation. As a result, biological drugs have very low bioavailability and short therapeutic half-lives. Fortunately, tools of chemistry and biotechnology have been developed into an elaborate arsenal, which can be applied to improve the pharmacokinetics of biological drugs. Depot-type release systems are available to achieve sustained release of drugs over time. Conjugation to synthetic or biological polymers affords long circulating formulations. Administration of biological drugs through non-parenteral routes shows excellent performance and the first products have reached the market. This Review presents the main accomplishments in this field and illustrates the materials and methods behind existing and upcoming successful formulations and delivery strategies for biological drugs.
通过重组技术生成的生物药物由于其高功效和高作用选择性而具有独特的地位。然而，这类治疗药物的主要缺点是其在口服给药和随后的循环过程中稳定性差。因此，生物药物的生物利用度非常低，治疗半衰期短。幸运的是，化学和生物技术的工具已经发展成为一个精心设计的武器库，可以应用于改善生物药物的药代动力学。储库型释放系统可实现药物随时间的持续释放。与合成或生物聚合物缀合可提供长效制剂。通过非肠外途径给予生物药物表现出优异的性能，并且第一批产品已经上市。本综述介绍了该领域的主要成就，并说明了现有和即将推出的生物药物成功制剂和传递策略背后的材料和方法。
