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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Development of propofol-loaded microemulsion systems for parenteral delivery
Hyun-Ki Ryoo1, Chun-Woong Park, Sang-Cheol Chi
1College of Pharmacy, Sungkyunkwan University, Suwon, Korea.
Archives of Pharmacal Research
|January 6, 2006
Summary
This study developed a stable aqueous parenteral formulation for propofol using oil-in-water (o/w) microemulsions. The optimized formulation demonstrated excellent stability and safety for intravenous administration.
Area of Science:
- Pharmaceutical Sciences
- Colloid and Surface Chemistry
Background:
- Propofol is a widely used intravenous anesthetic agent.
- Developing stable aqueous parenteral formulations for lipophilic drugs like propofol presents significant challenges.
- Microemulsion systems offer a promising approach to enhance drug solubility and stability.
Purpose of the Study:
- To develop a stable aqueous parenteral formulation of propofol using oil-in-water (o/w) microemulsion systems.
- To identify optimal surfactant and cosurfactant combinations for microemulsion formation.
- To evaluate the stability and hemocompatibility of the developed propofol microemulsion formulation.
Main Methods:
- Construction of pseudoternary phase diagrams to determine microemulsion composition.
- Screening of various surfactants and cosurfactants, including Solutol HS 15 and ethyl alcohol.
- Evaluation of formulation stability at 40°C for 8 weeks and assessment of propofol content.
- Hemolysis testing to determine the safety of the formulation on red blood cells.
Main Results:
- A stable o/w microemulsion region was achieved using a Solutol HS 15-ethyl alcohol (5/1) mixture.
- The optimized formulation containing 1% propofol and 8% surfactant mixture exhibited consistent droplet size (150 nm) and drug content over 8 weeks at 40°C.
- Hemolysis tests confirmed the formulation's non-toxicity to red blood cells.
Conclusions:
- Propofol can be successfully solubilized in aqueous parenteral formulations using o/w microemulsion systems.
- The developed microemulsion formulation demonstrates good physical stability and hemocompatibility, making it suitable for parenteral administration.
- This approach offers a viable strategy for formulating other lipophilic drugs for intravenous use.
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