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Magnetite-PLGA Microparticles for Oral Delivery of Insulin

  • Jianjun Cheng (a1), Christopher H. Yim (a1), Benjamin A. Teply (a1), Dennis Ho (a2), Omid C. Farokhzad (a3) (a4) and Robert S. Langer (a1)...
Abstract
Abstract

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-magnetitePLGA 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 Rmagnetite-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.

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