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

• Published in: Acta pharmaceutica Sinica. B Vol. 12; no. 2; pp. 621 - 636
• Main Authors: Bendicho-Lavilla, Carlos, Seoane-Viaño, Iria, Otero-Espinar, Francisco J., Luzardo-Álvarez, Asteria
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01-02-2022; Elsevier
• Subjects: Amylin mimetics; Biotherapeutics; Controlled-release formulations; Drug delivery systems; Exenatide; Glucagon-like peptide-1 receptor agonists; Microparticles; Nanoparticles; Peptide delivery; Review; Subcutaneous administration; Type 2 diabetes mellitus; Nanoparticles; Drug delivery systems; Biotherapeutics; Controlled-release formulations; Amylin mimetics; Subcutaneous administration; Type 2 diabetes mellitus; Glucagon-like peptide-1 receptor agonists; Exenatide; Microparticles; Peptide delivery
• ISSN: 2211-3835; 2211-3843
• DOI: 10.1016/j.apsb.2021.08.003

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.
This review summarises the current challenges of subcutaneous administration of peptide-based antidiabetics and provides an overview of the formulations available for the different routes of administration. [Display omitted]