Analytical techniques for structural characterization of proteins in solid pharmaceutical forms : an overview

Bolje, Aljoša (author), Gobec, Stanislav (author)

Therapeutic proteins as biopharmaceuticals have emerged as a very important class of drugs for the treatment of many diseases. However, they are less stable compared to conventional pharmaceuticals. Their long-term stability in solid forms, which is critical for product performance, depends heavily on the retention of the native protein structure during the lyophilization (freeze-drying) process and, thereafter, in the solid state. Indeed, the biological function of proteins is directly related to the tertiary and secondary structure. Besides physical stability and biological activity, conformational stability (three-dimensional structure) is another important aspect when dealing with protein pharmaceuticals. Moreover, denaturation as loss of higher order structure is often a precursor to aggregation or chemical instability. Careful study of the physical and chemical properties of proteins in the dried state is therefore critical during biopharmaceutical drug development to deliver a final drug product with built-in quality that is safe, high-quality, efficient, and affordable for patients. This review provides an overview of common analytical techniques suitable for characterizing pharmaceutical protein powders, providing structural, and conformational information, as well as insights into dynamics. Such information can be very useful in formulation development, where selecting the best formulation for the drug can be quite a challenge.

• Language: English
• Keywords: solid pharmaceuticals, lyophilization, analytical tools, protein characterization, protein structure, formulation development, antibody, excipients, stable drug product, safe drug
• Work type: Article
• Typology: 1.02 - Review Article
• Organization: FFA - Faculty of Pharmacy
• Publication status: Published
• Publication version: Version of Record
• Year: 2021
• Number of pages: 32 str.
• Numbering: Vol. 13, iss. 4, art. 534
• PID: 20.500.12556/RUL-135221
• UDC: 66.047.3:615.45
• ISSN on article: 1999-4923
• DOI: 10.3390/pharmaceutics13040534
• COBISS.SI-ID: 60765443
• Publication date in RUL: 01.03.2022

Record is a part of a journal

• Title: Pharmaceutics
• Shortened title: Pharmaceutics
• Publisher: MDPI
• ISSN: 1999-4923
• COBISS.SI-ID: 517949977

Licences

• License: CC BY 4.0, Creative Commons Attribution 4.0 International
• Link: http://creativecommons.org/licenses/by/4.0/
• Description: This is the standard Creative Commons license that gives others maximum freedom to do what they want with the work as long as they credit the author.
• Licensing start date: 11.04.2021

Secondary language

• Language: Slovenian
• Keywords: sušenje z zamrzovanjem, zgradba proteinov, stabilnost zdravil, pomožne snovi, terapevtske beljakovine, protitelesa, farmacevtske oblike

Projects

• Funder: Other - Other funder or multiple funders
• Funding programme: Republic of Slovenia, Ministry of Education, Science, and Sport
• Project number: 5442-1/2018/405

• Funder: ARRS - Slovenian Research Agency
• Project number: P1-0208
• Name: Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin