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Formulation development, characterization, and evaluation of bedaquiline fumarate - Soluplus® - solid dispersion
Vishwas P Pardhi1, Manisha Patel1, Keerti Jain1
1Department of Pharmaceutics, Drug Delivery and Nanomedicine Research Laboratory, National Institute of Pharmaceutical Education and Research (NIPER), Raebareli, India.
Pharmaceutical Development and Technology
|April 29, 2024
Summary
Bedaquiline fumarate (BQF) solubility and bioavailability were enhanced using Soluplus-based solid dispersions. Ternary solid dispersions significantly improved BQF
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Biopharmaceutics
Background:
- Bedaquiline fumarate (BQF) exhibits poor water solubility and dissolution, limiting its bioavailability due to its BCS Class II classification.
- Previous studies utilized crystalline polymers like poloxamer 188 for BQF solid dispersions, showing moderate solubility improvements.
- Amorphous polymers offer potential advantages for enhancing the solubility of poorly soluble drugs.
Purpose of the Study:
- To enhance the biopharmaceutical properties of bedaquiline fumarate (BQF).
- To develop and characterize binary (BSD) and ternary solid dispersions (TSD) of BQF using Soluplus®.
- To evaluate the impact of Soluplus® on BQF solubility, dissolution, cellular uptake, and bioavailability.
Main Methods:
- Preparation of binary solid dispersions (BSD) and ternary solid dispersions (TSD) of BQF with Soluplus®.
- Solubility and dissolution studies comparing BQF, BSD, and TSD.
- Solid-state characterization (e.g., FTIR) and cellular uptake studies in Caco-2 cell lines.
- Pharmacokinetic evaluation of the developed solid dispersion formulations.
Main Results:
- Solubility of BQF increased by 14.31-fold in BSD and 20.43-fold in TSD compared to pure BQF.
- Soluplus® demonstrated superior solubility enhancement for BQF compared to poloxamer 188.
- Characterization confirmed the amorphous state of BQF within the solid dispersions without chemical interactions.
- Enhanced cellular uptake and significantly improved pharmacokinetic profiles, including bioavailability, were observed for TSDs.
Conclusions:
- Solid dispersions formulated with amorphous Soluplus® represent a promising strategy for improving BQF's biopharmaceutical performance.
- Ternary solid dispersions (TSD) show superior potential for enhancing BQF solubility and bioavailability.
- This formulation approach offers a viable solution for overcoming the bioavailability challenges associated with poorly soluble drugs like BQF.
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