Guiding excipient selection for amorphous solid dispersions by combining an in vitro-in-silico approach – II: Supersaturation and drug release
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Author (Corporation)
Publication date
15.09.2025
Type of student thesis
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Type
01A - Journal article
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Parent work
International Journal of Pharmaceutics
Special issue
DOI of the original publication
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Series
Series number
Volume
682
Issue / Number
Pages / Duration
125976
Patent number
Publisher / Publishing institution
Elsevier
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Abstract
There is a growing industrial need for quick and early screening of amorphous solid dispersions (ASDs). While new technologies are emerging, including in-silico predictions and high-throughput experimentation, a significant gap exists due to a lack of comparative data. The aim of this work was thus to compare experimental data with calculations obtained by the Conductor like Screening Model for Real Solvents (COSMO-RS). A small-scale high throughput method based on solvent casting was used to evaluate the release behavior and precipitation inhibition capacity of ASDs of griseofulvin and nifedipine in the presence of ten pharmaceutically relevant polymers. COSMO-RS was then used to investigate the interaction strength between drug and polymer by means of drug activity coefficients. A stronger interaction would result in better supersaturation maintenance. This was reflected in our results and a good alignment between calculations and experimental performance was observed. COSMO-RS effectively differentiated between polymers with strong precipitation inhibition (PI) functionality and separated those with weaker efficacy for most of the ASDs studied. This pre-selected list of polymers can serve as a foundation for additional studies on all relevant drug development quality attributes, from stability to manufacturing.
Keywords
ASD dissolution, Precipitation inhibition, High-throughput, COSMO-RS, In vitro/in silico alignment
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ISBN
ISSN
0378-5173
1873-3476
1873-3476
Language
English
Created during FHNW affiliation
Yes
Strategic action fields FHNW
Publication status
Published
Review
Peer review of the complete publication
Open access category
Gold
License
Citation
Zeneli, E., Bohets, H., Mebenga, F. N., Tistaert, C., Holm, R., & Kuentz, M. (2025). Guiding excipient selection for amorphous solid dispersions by combining an in vitro-in-silico approach – II: Supersaturation and drug release. International Journal of Pharmaceutics, 682, 125976. https://doi.org/10.1016/j.ijpharm.2025.125976