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Optimization of preparative conditions for polylactide (PLA) microspheres containing ovalbumin
T Uchida1, K Yoshida, A Ninomiya
1Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Chemical & Pharmaceutical Bulletin
|September 1, 1995
Summary
Researchers optimized polylactide (PLA) microspheres for protein delivery. Smaller internal volumes and NaCl improved ovalbumin (OVA) loading, while smaller microspheres enhanced initial release, showing potential for long-acting delivery systems.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Polymer Chemistry
Background:
- Polylactide (PLA) microspheres are investigated for controlled protein delivery.
- Ovalbumin (OVA) serves as a model protein to evaluate encapsulation and release characteristics.
- The water-in-oil-in-water (w/o/w) emulsion solvent evaporation method is employed for microsphere preparation.
Purpose of the Study:
- To optimize the preparation of PLA microspheres for enhanced ovalbumin (OVA) loading and controlled release.
- To investigate the impact of various formulation parameters on microsphere characteristics.
- To assess the potential of PLA microspheres as a long-acting protein delivery system.
Main Methods:
- Optimization of internal aqueous phase volume and external NaCl concentration for improved OVA loading efficiency.
- Evaluation of OVA release profiles from PLA microspheres with varying molecular weights and lactide/glycolide (LA/GA) ratios.
- Analysis of the effect of microsphere particle size on initial burst release and long-term OVA retention.
Main Results:
- Reduced internal aqueous phase volume and addition of 2-10% NaCl significantly increased OVA loading efficiency.
- PLA microspheres exhibited an initial burst release followed by a sustained OVA release for at least 28 days.
- Lower molecular weight PLA and smaller microsphere diameters (e.g., 5.0 microns) led to faster initial release but retained significant OVA over 28 days.
Conclusions:
- Formulation parameters like internal phase volume, NaCl concentration, and PLA molecular weight critically influence OVA loading and release kinetics.
- PLA microspheres demonstrate potential as effective long-acting delivery systems for proteins.
- Particle size reduction can modulate initial release rates, offering tunable delivery profiles.