Oral Formulations of diclofenac beads and their Characterization
Diclofenac sodium (DS) is an effective non-steroidal anti-inflammatory drug (NSAID) agent. However, DS has short half life and adverse effects (e.g., ulcer bleeding or perforation of intestinal wall). The objectives of this study were to improve the oral bioavailability by loading DS in sodium alginate beads. The feasibility of different concentration and stabilizers on the mean particle size (MPS) and entrapment efficiency were also investigated.Materials and methods: DS-floating alginate or pectin beads were prepared by extrusion congealing technique. Physicochemical properties and particle size characterization were evaluated using Fourier Transform Infra-Red spectroscopy (FTIR), differential scanning calorimetry. Moreover, in vitro dissolution profiles were performed for all formulated DS loaded beads. Results: MPS of the prepared spherical beads of DS ranged from 568.3 ± 193 to 1791.3 ± 592 nm. and decreasing in sodium alginate or pectin concentration to the hydroxylpropylmethlycellulose ratio favored DS beads with a smaller MPS. There was a significant reduction in MPS, increment in drug content and drug release, with reduction of sodium alginate or pectin concentrations in the formulated beads. Both DSC and FTIR spectroscopy demonstrated a some sort of interaction between the drug and polymer used. Under conditions mimicking those in the stomach, a small amount of drug was released. The DS beads showed a release behavior dependent on pH value and alginate or pectin to hydroxypropylmethylcellulose ratio.