The objective of present project was to improve the dissolution profile of gliclazide by developing floating
alginate beads using various biodegradable polymers like gelatin, pectin and hydroxypropylmethylcellulose (HPMC). The
floating beads were prepared by a simple ionotropic gelatin method using calcium carbonate as gas generating agent. The
developed beads were characterized by Fourier transform infrared spectroscopy analysis, differential scanning calorimetry,
X-ray diffraction analysis and scanning electron microscopy (SEM). The prepared beads showed good in vitro floatation,
which was dependent on the concentration of gas-forming agent. SEM photomicrographs confirmed that the developed
beads were spherical in shape and had particle size in the range of 730 to 890 μm. The incorporation efficiency was
found to be in the range of 59.96 to 85.1%. The cumulative percent drug release from the beads after 10 h dissolution
study at pH 1.2 and pH 5.8 was in the range of 33 to 46% and 82 to 95% respectively. The concentration of the gas generating
agent was found to influence the release rate. The mechanism of drug release was Fickian diffusion with swelling.
The in vivo sub-acute hypoglycemic study in high fat diet induced diabetic C57BL/6J mice demonstrated significant (p <
0.05) hypoglycemic effect over a period of 12 h and 24 h, respectively, with HPMC and pectin beads. A significant (p <
0.05) reduction in fasting and non-fasting blood glucose levels, reduction in fasting plasma insulin level and a significant
improvement in glucose tolerance were observed in animals treated with formulations. The developed beads were suitable
carriers for improving the systemic absorption of gliclazide and maintaining reduced blood glucose levels.
Keywords: Alginate bead, Buoyancy, Floating bead, Gastroretentive, Gliclazide, Glucose tolerance, microencapsulation, potassium efflux.
Rights & PermissionsPrintExport