Polysaccharides are widely used in oral drug delivery systems because of the simplicity to obtain the desired drug delivery system and drug release profile, by the control of cross-linking, insolubility of crosslinked beads in gastric environment and broad regulatory acceptance. They include sodium alginate, pectin, chitosan, xantan gum, guar gum, starch, dextran, gellan (1-5). Among their various applications, polysaccharides are used for oral controlled release matrices, floating or bioadhesive sustained release beads or tablets, enteric coating, colon targeting of drugs and for pulsatile drug release (6-9). Pectin is an important ionic polysaccharide found in the plant cell wall, chemically made up of linear chains of partially methylated galacturonic acid units with an overall The purpose of this study was to improve the entrapment efficiency of the water-soluble drug metronidazole using internal cross-linking agents. Calcium pectinate beads containing metronidazole were prepared by dropping a drug-pectin solution in 1% and 5% (m/V) calcium chloride for surface cross-linked beads. For the core cross-linked beads calcium carbonate was dispersed in the drug-pectin solution. The beads were characterized by particle size, swelling ratio, SEM, DSC, and in vitro drug release. It was found that the beads obtained by core cross-linking produced more drug entrapped beads than the surface cross-linked beads. Beads obtained using 1% (m/V) calcium chloride showed more drug entrapment than these obtained using 5% calcium chloride. The core cross-linking of pectin beads reduced drug loss by about 10-20%. The water lodging capacity of beads depended upon gel strength which is a function of the internal gelling agent and pectin concentration. Complete drug release was observed within 30-60 min in the acidic dissolution medium. This work has showed that the core cross-linking agent increases the water-soluble drug entrapment in calcium pectinate beads.
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