Recent trends in stabilising peptides and proteins in pharmaceutical formulation – considerations in the choice of excipients

Abstract

In the area of peptide and protein pharmaceuticals, both the physical and chemical stability of biopharmaceuticals are critical and need to be optimised when formulating a drug product, in order to optimise the outcome after processing and storage. This review focuses on the effects on the stability from various types of excipient and the choices that have to be made during formulation of drug products containing peptides or proteins. It is illustrated, through examples, how the choice of one excipient over another can affect the stability of a protein drug formulation, along with other problems linked to this choice. The excipients used in pharmaceutical preparations are limited and from an academic point of view there is a clear requirement for new excipients.

High-Throughput Screening of Excipients Intended to Prevent Antigen Aggregation at Air-Liquid Interface

“…The excipients evaluated in this study were first selected based on their presence in marketed drugs for the parenteral route. While there is an urgent need for identifying new excipients from an academic point of view (41), using approved excipients limits development time by avoiding long and costly toxicological studies. Some excipient families were not included in this study, as their use was considered out of scope, e.g.…”

Purity profiling of Peptide Drugs

“…However, these excipients or impurities that are present in the excipients may also react with the peptides, inducing degradation [67,91,93,94]. Thus, it is crucial to select the most appropriate excipient [95,96].…”

Preventing Aggregation of Recombinant Interferon beta-1b in Solution by Additives: Approach to an Albumin-Free Formulation

“…[3][4][5] However, a universal formulation recipe does not work for all proteins. 6 When potential additives are identified, their concentration and use can be evaluated by screening assays for preventing aggregation of formulation. Human serum albumin (HSA) is usually used for formulation of IFN as a strong stabilizer.…”