Designing Formulation Strategies for Enhanced Stability of Therapeutic Peptides in Aqueous Solutions: A Review

Nugrahadi, Primawan Putra and Hinrichs, Wouter Leonardus Joseph and Frijlink, Henderik W. and Schoneich, Christian and Avanti, Christina (2023) Designing Formulation Strategies for Enhanced Stability of Therapeutic Peptides in Aqueous Solutions: A Review. Pharmaceutics, 15 (3). p. 935. ISSN 1999-4923

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Official URL / DOI: https://doi.org/10.3390/pharmaceutics15030935

Abstract

Over the past few decades, there has been a tremendous increase in the utilization of therapeutic peptides. Therapeutic peptides are usually administered via the parenteral route, requiring an aqueous formulation. Unfortunately, peptides are often unstable in aqueous solutions, affecting stability and bioactivity. Although a stable and dry formulation for reconstitution might be designed, from a pharmaco-economic and practical convenience point of view, a peptide formulation in an aqueous liquid form is preferred. Designing formulation strategies that optimize peptide stability may improve bioavailability and increase therapeutic efficacy. This literature review provides an overview of various degradation pathways and formulation strategies to stabilize therapeutic peptides in aqueous solutions. First, we introduce the major peptide stability issues in liquid formulations and the degradation mechanisms. Then, we present a variety of known strategies to inhibit or slow down peptide degradation. Overall, the most practical approaches to peptide stabilization are pH optimization and selecting the appropriate type of buffer. Other practical strategies to reduce peptide degradation rates in solution are the application of co-solvency, air exclusion, viscosity enhancement, PEGylation, and using polyol excipients.

Item Type: Article
Uncontrolled Keywords: therapeutic peptides; stabilization formulations; aqueous solutions
Subjects: R Medicine > R Medicine (General)
Divisions: Postgraduate Programs > Master Program in Clinical Pharmacy
Depositing User: Primawan Putra Nugrahadi, S. Farm., Apt.
Date Deposited: 20 Mar 2023 04:32
Last Modified: 12 Oct 2023 08:47
URI: http://repository.ubaya.ac.id/id/eprint/43577

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