Bendicho-Lavilla Carlos, Seoane-Viaño Iria, Otero-Espinar Francisco J, Luzardo-Álvarez Asteria
Department of Pharmacology, Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela (USC), Santiago de Compostela 15782, Spain.
Paraquasil Group, Health Research Institute of Santiago de Compostela (IDIS), Santiago de Compostela 15706, Spain.
Acta Pharm Sin B. 2022 Feb;12(2):621-636. doi: 10.1016/j.apsb.2021.08.003. Epub 2021 Aug 10.
Diabetes mellitus is a major health problem with increasing prevalence at a global level. The discovery of insulin in the early 1900s represented a major breakthrough in diabetes management, with further milestones being subsequently achieved with the identification of glucagon-like peptide-1 (GLP-1) and the introduction of GLP-1 receptor agonists (GLP-1 RAs) in clinical practice. Moreover, the subcutaneous delivery of biotherapeutics is a well-established route of administration generally preferred over the intravenous route due to better patient compliance and prolonged drug absorption. However, current subcutaneous formulations of GLP-1 RAs present pharmacokinetic problems that lead to adverse reactions and treatment discontinuation. In this review, we discuss the current challenges of subcutaneous administration of peptide-based therapeutics and provide an overview of the formulations available for the different routes of administration with improved bioavailability and reduced frequency of administration.
糖尿病是一个主要的健康问题，在全球范围内其患病率不断上升。20世纪初胰岛素的发现是糖尿病管理方面的一项重大突破，随后随着胰高血糖素样肽-1（GLP-1）的发现以及GLP-1受体激动剂（GLP-1 RAs）在临床实践中的引入，又取得了进一步的里程碑式进展。此外，生物治疗药物的皮下给药是一种成熟的给药途径，由于患者依从性更好且药物吸收时间延长，通常比静脉给药途径更受青睐。然而，目前GLP-1 RAs的皮下制剂存在药代动力学问题，导致不良反应和治疗中断。在本综述中，我们讨论了基于肽的治疗药物皮下给药当前面临的挑战，并概述了可用于不同给药途径的制剂，这些制剂具有更高的生物利用度和更低的给药频率。
