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Protein Based Amorphous Solid Dispersion: a Case Study Investigating Different Whey Proteins at High Drug Loading
Donglei Leng1, Bulut Bulduk1, Toni Widmer2
1Zerion Pharma A/S, Fruebjergvej 3, 2100, Copenhagen, Denmark.
Pharmaceutical Research
|May 26, 2023
Summary
Whey protein isolate (WPI) and its components show potential for amorphous solid dispersions (ASDs) with poorly soluble drugs. Beta-lactoglobulin (BLG) demonstrated superior stability and dissolution enhancement at high drug loadings up to 70%.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Biochemistry
Background:
- Whey protein isolate (WPI) is a promising excipient for amorphous solid dispersions (ASDs) at 50% drug loading.
- WPI comprises beta-lactoglobulin (BLG), alpha-lactalbumin (ALA), and casein glycomacropeptides (CGMP), but their individual roles in ASD performance are unknown.
- The performance of WPI-based ASDs at drug loadings exceeding 50% remains unexplored.
Purpose of the Study:
- To investigate the individual contributions of BLG, ALA, and CGMP to ASD performance.
- To evaluate ASDs formulated with WPI and its components at high drug loadings (50%, 60%, and 70%).
- To assess the feasibility of developing ASDs with poorly water-soluble drugs (Compound A and Compound B) at increased loadings.
Main Methods:
- Formulation of ASDs using BLG, ALA, CGMP, and WPI with Compound A and Compound B at 50%, 60%, and 70% drug loadings.
- Solid-state characterization of the formulated ASDs.
- Analysis of dissolution rates and physical stability of the ASDs.
Main Results:
- All ASD formulations were amorphous and exhibited enhanced dissolution rates compared to their crystalline drug counterparts.
- BLG-based ASDs, particularly for Compound A, showed superior performance in terms of physical stability, dissolution enhancement, and solubility increase.
- The study successfully developed amorphous solid dispersions at drug loadings up to 70%.
Conclusions:
- Whey proteins, including individual components like BLG, are effective excipients for developing amorphous solid dispersions (ASDs).
- ASDs can be successfully developed with poorly water-soluble drugs at high drug loadings up to 70%.
- BLG emerges as a particularly promising component for enhancing the stability and dissolution of ASDs.
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