Patel, Nachiket, et al. Progress in biomaterials 5.2 (2016): 117-133.
Calcium alginate beads serve as a biodegradable, pH-sensitive multiparticulate delivery system for the oral administration of ceftriaxone sodium (CS), a highly water-soluble and acid-labile antibiotic. Formed via ionotropic gelation of sodium alginate with calcium chloride, the crosslinked hydrogel matrix protects the drug from gastric degradation and enables sustained intestinal release. Incorporation of secondary polymers and enteric coating further modulates release kinetics and enhances entrapment efficiency.
Bead Preparation and Optimization: CS-loaded beads were prepared by extruding sodium alginate solutions (with or without sodium carboxymethylcellulose, acacia, or HPMC) into aqueous CaCl2 solution. Beads were cured, dried, and subsequently coated with cellulose acetate phthalate (CAP) for enteric protection.
Physicochemical Characterization: Optimal formulation F9 (sodium alginate/CMC/CAP) achieved 75 ± 5% drug entrapment efficiency, with particle size of 1.59 ± 0.15 mm. TGA revealed enhanced thermal stability for alginate-CMC beads, with reduced weight loss at elevated temperatures. AFM and SEM showed rough, porous surfaces for uncoated beads, while CAP coating produced smoother surfaces with reduced roughness. Swelling indices ranged from 0.9 to 3.4 in SGF (pH 1.2).
Release Performance: In vitro release studies demonstrated that CAP-coated beads released 35–47% of CS in SGF over 2 h, with sustained release in SIF (pH 6.8) for up to 18 h. Release kinetics followed first-order models via non-Fickian diffusion and erosion mechanisms, with n values of 0.15–0.46 indicating anomalous transport.