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Formulation of parenteral microemulsion containing itraconazole
Yun-Seok Rhee1, Chun-Woong Park, Tae-Young Nam
1College of Pharmacy, Sungkyunkwan University, Suwon 440-746, Korea.
Archives of Pharmacal Research
|March 3, 2007
Summary
This study developed a novel itraconazole (ITZ) parenteral formulation using an oil-in-water microemulsion. The optimized ITZ microemulsion demonstrated good stability and safety, showing potential for intravenous drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Itraconazole (ITZ) is an antifungal agent with poor aqueous solubility, limiting its parenteral administration.
- Developing stable and effective parenteral formulations is crucial for treating systemic fungal infections.
Purpose of the Study:
- To develop a stable aqueous parenteral formulation of itraconazole (ITZ) using an oil-in-water (o/w) microemulsion.
- To evaluate the suitability of the developed microemulsion for parenteral administration.
- To compare the pharmacokinetic profile of the ITZ microemulsion with existing formulations in rats.
Main Methods:
- Construction of pseudoternary phase diagrams to determine optimal microemulsion components (oil, surfactant, cosurfactant).
- Evaluation of microemulsion characteristics including droplet size analysis and hemolysis tests.
- Pharmacokinetic studies in rats comparing the ITZ microemulsion with PEG 400 solution and cyclodextrin formulations.
Main Results:
- An optimized o/w microemulsion formulation for ITZ was successfully developed.
- The microemulsion exhibited an average droplet size below 150 nm and demonstrated non-toxicity to red blood cells via hemolysis testing.
- The ITZ microemulsion showed promising pharmacokinetic profiles in rats compared to other tested formulations.
Conclusions:
- The developed itraconazole microemulsion is a suitable and safe candidate for parenteral drug delivery.
- This formulation offers a potential improvement over existing parenteral itraconazole options.
- Further investigation into this microemulsion system could advance antifungal parenteral therapy.
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