Evaluation of Aceclofenac Loaded Alginate Mucoadhesive Spheres Prepared by Ionic Gelation

Abstract


 Controlled release aceclofenac spheres were prepared in a cross-linked alginate matrix using ionotropic gelation technique. A suspension of aceclofenac in sodium alginate solution was added drop wise into 10% w/v calcium chloride solution and the resulting spheres were evaluated for their drug content, flow properties, mucoadhesive property and the dissolution rate. The aceclofenac loaded alginate spheres were prepared using various mucoadhesive polymers: sodium alginate, HPMC, sodium CMC, guar gum, methyl cellulose and carbopol. The calcium chloride was used as the crosslinking agent. Fourier transform infrared spectroscopy (FTIR) was used to evaluate the drug-polymer interaction. The alginate spheres showed good rheological properties, drug content uniformity and high entrapment efficiency. The aceclofenac release from the spheres was slow and extended up to 10 hours. The drug loaded spheres exhibited good mucoadhesive property in the in vitro wash off test. The drug release from the optimized formulation (drug-sodium alginate-HPMC K15M; 1:0.9: 0.1 ratio) followed zero order kinetics and exhibited non-Fickian diffusion. The rate of release of aceclofenac decreased with increasing concentration of sodium alginate due to slow penetration of dissolution fluid in the spheres. The results suggest that alginate spheres can potentially deliver aceclofenac at zero-order controlled release following oral administration. The FTIR studies indicated the absence of the drug-polymer interaction in the solid state.