Insulin loaded eudragit L100 microspheres for oral delivery: preliminary in vitro studies

Abstract

Eudragit L100 microspheres were prepared using water-in-oil-in water (w/o/w) emulsion-solvent evaporation with polysorbate 20 as dispersing agent in the internal aqueous phase, and PVA/PVP as stabilizer in the external aqueous phase. Smaller internal and external aqueous phases provided higher drug encapsulation. The PVA-stabilized microspheres having maximum drug encapsulation (84.5 2.8%) released 7% insulin at pH 1.0 in 2 h. In phosphate buffer (pH 7.4), microspheres showed an initial burst release of 21% in 1 h with additional 35% release in the next 5 h. The smaller the volumes of internal and external aqueous phases, the lower the initial burst release. The release of drug from microspheres followed Higuchi kinetics. Scanning electron microscopy of PVA stabilized microspheres demonstrated spherical particles with smooth surface and laser diffractometry revealed a mean particle size (V(m)) of 59.11 30 m.