Fighting type 2 diabetes: Formulation strategies for peptide-based therapeutic

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.

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Article information: Carlos Bendicho-Lavilla, Iria Seoane-Viaño, Francisco J. Otero-Espinar, Asteria Luzardo-Álvarez, Fighting type 2 diabetes: Formulation strategies for peptide-based therapeutics, Acta Pharmaceutica Sinica B, 2021. https://doi.org/10.1016/j.apsb.2021.08.003.