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Published on: January 7, 2019
Liquid antisolvent precipitation process for solubility modulation of bicalutamide.
Tarique Ali Meer1, Kiran P Sawant, Purnima D Amin
1Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Matunga, Mumbai-400019 India.
Acta Pharmaceutica (Zagreb, Croatia)
|December 29, 2011
Summary
The liquid antisolvent process improved bicalutamide solubility and dissolution. This method enhances the bioavailability of poorly soluble drugs like bicalutamide using hydrophilic polymers and surfactants.
Area of Science:
- Pharmaceutics
- Materials Science
Background:
- Bicalutamide exhibits poor aqueous solubility and dissolution, leading to variable oral bioavailability.
- Enhancing solubility is crucial for improving the therapeutic efficacy of poorly water-soluble drugs.
Purpose of the Study:
- To modify the solubility of bicalutamide using the liquid antisolvent precipitation process.
- To optimize the process parameters for effective solubility enhancement.
Main Methods:
- Exploration of the liquid antisolvent process as a solubility modulation tool.
- Selection of Hydroxypropyl Methylcellulose E5 (HPMC E5) as a hydrophilic polymer and Poloxamer 407 as a surfactant.
- Optimization of hydrophilic polymer, surfactant, and drug loading concentrations.
- Characterization of resultant microcrystals using IR, DSC, SEM, XRD, particle size analysis, and specific surface area determination.
- Evaluation of dissolution kinetics.
Main Results:
- Successful modification of bicalutamide solubility and dissolution characteristics via liquid antisolvent precipitation.
- Characterization confirmed the formation of microcrystals with altered material properties.
- Optimized process parameters led to improved drug solubility.
Conclusions:
- The liquid antisolvent process is an effective method for enhancing the solubility and dissolution of poorly water-soluble drugs like bicalutamide.
- This approach holds potential for improving the bioavailability and therapeutic outcomes of bicalutamide.
- Further investigation into the formulation and in vivo performance is warranted.
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