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A novel self emulsifying parenteral drug delivery system
PDA Journal of Pharmaceutical Science and Technology
|February 7, 2001
Summary
Glycerol enables the creation of novel parenteral self-emulsifying drug delivery systems (PSEDDS) by forming isotropic liquids. Other polyhydroxy alcohols like propylene glycol and sorbitol were less effective in PSEDDS formulations.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Formulation Science
Background:
- Parenteral emulsion formulations require effective emulsifiers for stability and drug delivery.
- Polyhydroxy alcohols are explored for their potential to enhance emulsion properties.
Purpose of the Study:
- To investigate the impact of glycerol, propylene glycol, and sorbitol on parenteral emulsion formulations.
- To evaluate the potential of these polyols in creating self-emulsifying systems for parenteral drug delivery.
Main Methods:
- Soybean oil-in-water emulsions were prepared with varying concentrations of lecithin, Span 20, and polyhydroxy alcohols.
- Characterization of self-emulsifying properties, isotropic liquid formation, and particle size reduction was performed.
- A model drug (lidocaine) was incorporated into a PSEDDS formulation to assess spontaneous emulsification.
Main Results:
- Glycerol at 30% or higher concentrations, with lecithin and Span 20, formed self-emulsifying isotropic liquids.
- These isotropic liquids spontaneously emulsified in water to submicron particle sizes (0.39-0.4 micron).
- Propylene glycol and sorbitol, or lower glycerol concentrations, did not yield self-emulsifying mixtures, with varying particle size reduction efficiencies.
Conclusions:
- Glycerol is effective in developing parenteral self-emulsifying drug delivery systems (PSEDDS).
- The concentration of polyhydroxy alcohol significantly influences self-emulsification and particle size.
- Polyhydroxy alcohols alter surfactant distribution at the interface, impacting emulsion characteristics.