A Comparative Study between A Protein Based Amorphous Formulation and Other Dissolution Rate Enhancing Approaches: A Case Study with Rifaximin
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Amorphous solid dispersions (ASDs) based on proteins as co-formers have previously shown promising potential to improve the solubility and bioavailability of poorly water-soluble drugs. In particular, whey proteins have shown to be promising co-formers and amorphous stabilizers in ASD formulations, including at high drug loading. In this study, the feasibility of the whey protein β-lactoglobulin (BLG) as a co-former in ASDs was compared to the more traditional ASD co-formers based on synthetic polymers (hydroxypropyl methylcellulose acetate succinate and Eudragit® L) as well as to a nanocrystalline formulation. The poorly water-soluble drug rifaximin (RFX) was chosen as the model drug. All drug/co-former formulations were prepared as fully amorphous ASDs by spray drying at 50% (w/w) drug loading. The BLG-based ASD had the highest glass transition temperature and showed a faster dissolution rate and higher drug solubility in three release media with different pH values (1.2, 4.5, and 6.5) compared to the polymer-based ASDs and the nanocrystalline RFX. In conclusion, BLG is a promising co-former and amorphous stabilizer of RFX in ASD formulations, superior to the selected polymer-based ASD systems or the nanocrystalline formulation.
Original language | English |
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Article number | 126 |
Journal | Pharmaceutics |
Volume | 15 |
Issue number | 1 |
Number of pages | 10 |
ISSN | 1999-4923 |
DOIs | |
Publication status | Published - 2023 |
Bibliographical note
Funding Information:
X.Z. would like to thank the China Scholarship Council (CSC No: 201908210313) for financial support. Arla Foods Ingredients Group P/S is thanked for providing the samples of Lacprodan BLG Pharma Grade. ®
- amorphous solid dispersion, dissolution, nanocrystal, polymer, β-lactoglobulin
Research areas
ID: 336124310