Preparation and in vitro characterization of AL-Beads containing carbamazepine and/or levetiracetam

Abstract

The purpose of the present study was to prepare only levetiracetam (LEV) or carbamazepine (CBZ) or their combination (LEV+CBZ)-loaded alginate (AL) beads for oral administration to treat epilepsy and to evaluate their in vitro characteristics. AL beads were prepared using ionotropic gelation method and lyophilized. The bead formulations were evaluated for particles size, surface morphology, encapsulation efficiency and in vitro drug release in PB pH 6.8 and HCl pH 1.2 release mediums. FT-IR was also used to characterize the beads. The mean particle sizes of wet and lyophilized AL beads were in range of 1.609±0.073-1.779±0.078 mm and 1.075±0.182-1.275±0.138 mm, respectively. The encapsulation efficiency (EE%) values of bead formulations were in the range of 18.74-24.65% for LEV and 90.36-94.03% for CBZ. The pH of the medium affects the swelling behaviours of AL beads and the degree of swelling of AL beads increased with increase of pH of release medium, due to exchange of the Ca 2+ ion with Na + . Besides, the pH of the release medium and the high water solubility of LEV affected the drug release rate from beads. AL beads might be useful to use for oral administration of LEV and CBZ to obtain additive/synergistic effect in a combined treatment of epilepsy.Wt: the weight of beads at time (mg); W0: the initial weight of beads (mg).The experiments were carried out in triplicate and data as average was given. Uğur et al. Alginate beads containing LEV+CBZ