Preparation of biodegradable microspheres containing water-soluble drug, β-lactam antibiotic

Poly (l-lactic acid) (PLLA) microspheres loaded with ampicillin sodium (AMP-Na), β-lactam antibiotic, were prepared by a w/o/w multiple emulsion-solvent evaporation method. The amounts of each component in three phases (inner water phase, organic phase, and outer water phase) were carefully examined in the preparation of PLLA microspheres. The stirring rate, another preparation parameter, was also investigated for study on the effect of mechanical stress on the drug loading and morphology of PLLA microspheres. Most of the preparation parameters had a great influence on the drug loading, surface morphology and size distribution of PLLA microspheres. PLLA microspheres with 15.89 w/w% drug loading were subjected to the in vitro release experiment. The release of ampicillin sodium was constant at a rate of 1.68 μg/ml/day per 1 mg of microspheres for 18 days after a 4 days initial burst effect.