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Calcium alginate/gum Arabic beads containing glibenclamide: Development and in vitro characterization

Nayak, Amit Kumar, Das, Biswarup, Maji, Ruma
International journal of biological macromolecules 2012 v.51 no.5 pp. 1070-1078
Fourier transform infrared spectroscopy, calcium alginate, drugs, encapsulation, gelation, glibenclamide, gum arabic, models, pH, patient compliance, response surface methodology, scanning electron microscopy, sodium alginate
This work investigates the development, optimization and in vitro characterization of calcium alginate/gum Arabic beads by an ionotropic gelation method for prolonged sustained release of glibenclamide. The effects of amount of sodium alginate and gum Arabic as independent process variables on the drug encapsulation efficiency and drug release were optimized and analyzed based on central composite design and response surface methodology. Increment in drug encapsulation efficiency and decrease in drug release were found with the increase of both the amounts of sodium alginate and gum Arabic, used as polymer-blend. These optimized beads showed high drug encapsulation efficiency (86.02±2.97%), and suitable sustained drug release pattern over prolonged period (cumulative drug release after 7h of 35.68±1.38%). The average size of these formulated dried beads containing glibenclamide ranged from 1.15±0.11 to 1.55±0.19mm. The in vitro dissolution of these beads showed prolonged sustained release of glibenclamide over 7h, which followed first-order model (R²=0.9886–0.9985) with anomalous (non-Fickian) diffusion mechanism (release exponent, n=0.72–0.81). The swelling and degradation of the optimized beads were influenced by pH of test mediums. These beads were also characterized by SEM and FTIR spectroscopy for surface morphology and excipients-drug interaction analysis, respectively. These developed calcium alginate/gum Arabic beads containing glibenclamide could possibly be advantageous in terms of advanced patient compliance with reduced dosing interval.