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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Influence and effect of osmolytes in biopharmaceutical formulations

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Wlodarczyk, Samarina R. [1] ; Custodio, Debora [1] ; Pessoa Jr, Adalberto ; Monteiro, Gisele [2]
Total Authors: 4
[1] Univ Sao Paulo, Fac Pharmaceut Sci, Dept Biochem & Pharmaceut Technol, BR-05434070 Sao Paulo, SP - Brazil
[2] Pessoa Jr, Jr., Adalberto, Univ Sao Paulo, Fac Pharmaceut Sci, Dept Biochem & Pharmaceut Technol, BR-05434070 Sao Paulo, SP - Brazil
Total Affiliations: 2
Document type: Journal article
Web of Science Citations: 5

Osmolytes are small organic molecules accumulated by cells in response to environmental stresses. They are represented by amino acids, sugars, polyols, tertiary sulphonium and quaternary ammonium compounds. These molecules present a protective behaviour and favour the equilibrium of macromolecules towards the native form, preventing denaturation and promoting the folding of unfolded proteins. Protein formulations due to their biological character require greater care during the manufacturing process, shelf-life and administration of the drug, as variations in these factors may result in denaturation, inactivation and/or protein aggregation. These drawbacks can be surpassed using osmolytes as excipients in protein formulations as stabilisers, bulking agents and even buffers. A number of 133 biologics, including vaccines and immunoglobulins, approved by the U.S. Food and Drug Administration (FDA) between 1998 and 2017 were analysed in this work in order to identify the most used group of osmolyte molecules. A deep insight into their role in protein formulations was discussed and compared to data in the literature. The advantages and disadvantages of their use in specific formulations were also extensively discussed here. In conclusion, investigation into the role of osmolytes in each formulation is essential for understanding their effect and provides a background to be used when selecting the best osmolyte to fit a specific formulation without excluding the patient needs. (AU)

FAPESP's process: 15/07749-2 - Protein engineering and comparison of microbial expression systems of the biopharmaceutical L-asparaginase
Grantee:Gisele Monteiro
Support type: Regular Research Grants
FAPESP's process: 13/08617-7 - Production of extracellular L-asparaginase: from bioprospecting to the engineering of an antileukemic biopharmaceutical
Grantee:Adalberto Pessoa Junior
Support type: Research Projects - Thematic Grants
FAPESP's process: 13/24024-6 - Effects of protein-aqueous medium interactions on structural modifications of L-asparaginase II of Escherichia coli
Grantee:Samarina Rodrigues Wlodarczyk
Support type: Scholarships in Brazil - Doctorate
FAPESP's process: 15/24463-5 - Characterization of L-asparaginase of Erwinia chysanthemi improved by synthetic evolution of proteins and optimization of production conditions
Grantee:Débora Fernandes Custodio
Support type: Scholarships in Brazil - Doctorate (Direct)