Modification of release and penetration behavior of water-soluble active ingredient from ball-milled glutinous starch matrix via carboxymethylcellulose blending

Abstract

This present work describes the possible advantages of carboxymethylcellulose (CMC) blending with ball-milled glutinous starch (BMGS) on the modification of release and penetration of model water-soluble active ingredient, lidocaine hydrochloride, from the blended matrix. The 20–67% CMC mass containing CMC-BMGS matrices were fabricated by casting the aqueous dispersion of CMC-BMGS onto the tray and oven-dried. BMGS and CMC were compatible as revealed by SEM and ATR-FTIR. Irrespective of the CMC mass, all CMC-BMGS matrices showed comparable matrix mass, thickness, moisture content, moisture absorption as well as mechanical and mucoadhesive properties. The surface pH of CMC-BMGS tended to increase with the CMC mass. Depends on CMC mass, matrix properties, release, and penetration rates were modulated significantly. CMC had shown a substantial role in the swelling and erosion behaviors of BMGS films, and thus modulated the release and penetration significantly. The release and penetration mechanisms of active ingredient from the CMC-BMGS matrices were Fickian diffusion-controlled, with rates of release and penetration ranging from 2.05 ± 0.21 to 7.55 ± 1.08%/min½, and from 3.48 ± 0.28 to 8.04 ± 0.64 μg/cm2/min½, respectively. The capability of CMC-BMGS matrices as mucoadhesive delivery systems to provide sustained delivery of water-soluble active ingredients was disclosed.