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Published on: August 9, 2022
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β-Lactoglobulin-based amorphous solid dispersions: A graphical review on the state-of-the-art
Xuezhi Zhuo1, Ieva Jasiukenaite1, Korbinian Löbmann1
1Zerion Pharma A/S, Fruebjergvej 3, 2100 Copenhagen, Denmark.
Summary
Whey protein isolate, specifically beta-lactoglobulin (BLG), shows promise for creating amorphous solid dispersions (ASDs) that enhance drug solubility and oral bioavailability. BLG-based ASDs offer effective amorphous stabilization and improved drug dissolution compared to traditional polymers.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Biochemistry
Background:
- Proteins are emerging as novel excipients for amorphous solid dispersions (ASDs).
- Beta-lactoglobulin (BLG), a whey protein isolate, demonstrates potential for stabilizing amorphous drugs and enhancing solubility.
- High drug loadings (≥50 wt%) are achievable with BLG-based ASDs.
Purpose of the Study:
- To provide a comprehensive graphical review of recent findings on BLG-based ASDs.
- To compare the dissolution performance of BLG-based ASDs with traditional polymer-based ASDs.
- To elucidate the mechanisms of amorphous stabilization and drug solubility enhancement by BLG.
Main Methods:
- Comparative analysis of dissolution performance.
- Summary of drug loading and amorphous stabilization mechanisms.
- Description of drug-BLG interactions in solution.
- Investigation of spray drying effects on BLG secondary structure and ASD performance.
Main Results:
- BLG-based ASDs exhibit competitive dissolution performance compared to polymer-based ASDs.
- BLG effectively stabilizes amorphous drugs at high drug loadings.
- Drug-BLG interactions in solution enhance drug solubility.
- Spray drying influences BLG's secondary structure, impacting stabilization and dissolution.
Conclusions:
- BLG is a viable and effective excipient for amorphous solid dispersions.
- Understanding BLG's structural and interactional properties is key to optimizing ASD performance.
- BLG-based ASDs offer a promising strategy for improving oral bioavailability of poorly soluble drugs.
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