SUSTAINED-RELEASE SYSTEM FOR EPO AND GM-CSF

摘要

This patent disclosed sustained-release microsphere dosage forms of EPO and GM-CSF respectively and methods for their preparation. The proteins are first loaded in solvent-resistant polysaccharide particles using a stabilized aqueous-aqueous emulsion consisting of polysaccharide dispersed phase and polyethylene glycol (PEG) continuous phase, followed by freeze-drying. This particle forming process avoids exposing proteins to water-oil or water-air (or intra-particle cross-linking reagent), factors known to denature proteins. The lyophilized powder was then washed using organic solvent to remove the PEG continuous phase. The proteins loaded in the solvent-resistant polysaccharide particles can easily be sustained-release microsphere formulation without denaturing, aggregation, adsorption and deactivation.