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Preparation of polymeric microcapsules: formulation studies.
K Bjerknes1, K Dyrstad, G Smistad
1Nycomed Imaging AS, Oslo, Norway.
Drug Development and Industrial Pharmacy
|July 20, 2000
Summary
Researchers developed air-filled microcapsules using biodegradable polyester and a new poly(ethylene glycol) surfactant. Mannitol addition improved freeze-drying stability and suspension yield for these microcapsules.
Area of Science:
- Materials Science
- Chemical Engineering
- Pharmaceutical Technology
Background:
- Air-filled microcapsules are prepared using oil-in-water emulsions with biodegradable polyesters.
- Previous work utilized human serum albumin as a surfactant.
- This study explores a new poly(ethylene glycol) (PEG) block copolymer as a surfactant replacement.
Purpose of the Study:
- To optimize the formulation of air-filled microcapsules for improved suspension and emulsion stability during production.
- To evaluate the efficacy of a novel PEG-based block copolymer as a surfactant.
- To investigate the impact of formulation parameters on microcapsule characteristics.
Main Methods:
- Factorial design was employed to study formulation parameters like mannitol, polymer, and surfactant concentrations, pH, and phase ratio.
- Ordinary least-square (OLS) and partial least-square regression (PLSR) were used for data analysis.
- Emulsion stability was assessed at 60°C.
Main Results:
- The PEG block copolymer proved to be a suitable alternative to human serum albumin.
- Emulsion stability at 60°C was significantly influenced by polymer and surfactant concentrations.
- Low polymer concentrations (< 5% w/v in (-)-camphene) yielded the highest microcapsule production.
- Mannitol addition enhanced freeze-drying protection, reducing cracks and shrinkage, and increasing suspension yield.
Conclusions:
- A novel PEG-based surfactant effectively replaces human serum albumin in air-filled microcapsule production.
- Optimized concentrations of polymer and surfactant are crucial for emulsion stability and microcapsule yield.
- Mannitol is a key excipient for improving freeze-drying stability and the quality of the final microcapsule product.