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Solubilizing poorly soluble antimycotic agents by emulsification via a solvent-free process
Aslihan Akkar1, Pawel Namsolleck, Michael Blaut
1Free University of Berlin, Department of Pharmaceutical Technology, Biotechnology and Quality Management, Kelchstrasse 31, 12169 Berlin, Germany.
AAPS Pharmscitech
|June 17, 2004
Summary
Solubilization by emulsification (SolEmuls) technology successfully formulated itraconazole and ketoconazole into parenteral emulsions. This cost-effective method yields stable, injectable drug formulations for antimycotic agents.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Formulation Science
Background:
- Parenteral administration of antifungal drugs like itraconazole and ketoconazole requires stable oil/water emulsions.
- Traditional formulation methods can be complex and costly.
- SolEmuls (solubilization by emulsification) offers a solvent-free approach for creating such emulsions.
Purpose of the Study:
- To formulate itraconazole and ketoconazole as stable oil/water emulsions for parenteral delivery using SolEmuls technology.
- To evaluate drug-loading capacity, physical stability, and dissolution of the formulated emulsions.
- To assess the applicability of SolEmuls for antimycotic agents.
Main Methods:
- Utilized SolEmuls technology, a solvent-free homogenization process.
- Incorporated itraconazole and ketoconazole into Lipofundin MCT 20% emulsion.
- Investigated the effects of lecithin and Tween 80 as stabilizers.
- Assessed drug loading, physical stability, and dissolution.
Main Results:
- Achieved complete dissolution of itraconazole up to 10.0 mg/mL; hybrid dispersion at 20 mg/mL.
- Itraconazole emulsions demonstrated physical stability for 9 months.
- Ketoconazole emulsions showed instability with lecithin alone; stabilization achieved with added Tween 80.
- Ketoconazole emulsions (1 mg/mL) stabilized with 2.0% Tween 80 were stable for 6 months.
Conclusions:
- SolEmuls technology is effective for formulating parenteral emulsions of itraconazole and ketoconazole.
- The method provides a cost-effective and scalable approach for producing injectable antimycotic formulations.
- SolEmuls is a versatile technology applicable to various challenging drug molecules for parenteral delivery.