A Comparative Study between A Protein Based Amorphous Formulation and Other Dissolution Rate Enhancing Approaches: A...

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Biotechnology

Background:

• Amorphous solid dispersions (ASDs) enhance solubility and bioavailability of poorly water-soluble drugs.
• Whey proteins, particularly beta-lactoglobulin (BLG), show potential as co-formers and stabilizers in ASDs, even at high drug loadings.

Purpose of the Study:

• To evaluate the feasibility of beta-lactoglobulin (BLG) as a co-former in amorphous solid dispersions (ASDs).
• To compare BLG-based ASDs with traditional synthetic polymer ASDs and a nanocrystalline formulation using rifaximin (RFX) as a model drug.

Main Methods:

• Preparation of fully amorphous ASDs using spray drying at 50% (w/w) drug loading.
• Formulations included BLG, synthetic polymers (hydroxypropyl methylcellulose acetate succinate, Eudragit® L), and nanocrystalline RFX.
• Evaluation of drug solubility and dissolution rates in release media at pH 1.2, 4.5, and 6.5.

Main Results:

• The BLG-based ASD exhibited the highest glass transition temperature.
• BLG-ASD showed significantly faster dissolution rates and higher drug solubility across different pH values compared to polymer-based ASDs and nanocrystalline RFX.
• All formulations were successfully prepared as fully amorphous ASDs at 50% drug loading.

Conclusions:

• Beta-lactoglobulin (BLG) is a highly effective co-former and amorphous stabilizer for rifaximin (RFX).
• BLG-based ASDs offer superior performance in terms of solubility and dissolution compared to conventional polymer-based ASDs and nanocrystalline formulations.
• This study highlights the potential of protein-based ASDs as an advanced drug delivery strategy.