Technology development to evaluate the effectiveness of viscosity reducing excipients

Addition of pharmaceutical excipients is a commonly used approach to decrease the viscosity of highly concentrated protein formulations, which otherwise could not be subcutaneously injected or processed. The variety of protein–protein interactions, which are responsible for increased viscosities, makes a portfolio approach necessary. Screening of several excipients to develop such a portfolio is time and money consuming in industrial settings.

Highlights

• Protein-protein interactions responsible for increased viscosities of highly concentrated protein formulations were investigated using dynamic light scattering.

• Qualitative correlation between protein–protein interactions and high-concentration viscosity behavior could be shown.

• Gained insights support the development of novel highly concentrated protein formulations.

Responsible protein–protein interactions were investigated using the interaction parameter k_D obtained from dynamic light scattering measurements in the studies presented herein. Together with in-silico calculated excipient parameter, k_D could be used as a screening tool accelerating screening and formulation development as k_D is suitable to high-throughput formats using small quantities of protein and low concentrations. A qualitative correlation between k_D and high-concentration viscosity behavior could be shown in our case.

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Niels Banik, Stefan Braun, Jan Gerit Brandenburg, Gert Fricker, Devendra S. Kalonia, Tobias Rosenkranz,
Technology development to evaluate the effectiveness of viscosity reducing excipients, International Journal of Pharmaceutics, Volume 626, 2022, 122204, ISSN 0378-5173, https://doi.org/10.1016/j.ijpharm.2022.122204