Magnetite-PLGA microparticles for oral delivery of insulin

Magnetic responsive particles were designed for use in oral delivery of insulin. Magnetite nanoparticles (12 nm average size) were synthesized and co-encapsulated with insulin into poly(lactide-co-glycolide) (PLGA) microparticles (4.6 ± 2.2 μm average particle size) through the double-emulsion method, The spherical structures of resulting microparticles were well maintained at magnetite content 5 wt % or less. Mice were gavaged with ¹²⁵I-insulin-magnetite-PLGA microparticles and a circumferential trans-abdominal magnetic field was applied forty minutes after administration to retard the transit of the microparticles in the intestinal tract. As control, mice were similarly dosed without the subsequent trans-abdominal magnetic field. Mice were sacrificed, and the intestinal radioactivity was 101% and 145% higher in treated mice versus the control at 6 h and 12 h, respectively. A single administration of 50 unit/kg Humulin R-magnetite-PLGA microparticles to the fasted mice resulted in 66% reduction of blood glucose level in the presence of external magnetic field at 12 h, compared to 27% reduction in the absence of magnetic field,