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A Novel Approach to Study Enzymatic Degradation of Ter-polymeric Beads for Gastrointestinal Drug Delivery: Synthesis and Characterization

Polymer Research Laboratory, Department of Chemistry, Government Model Science College (Autonomous), Jabalpur (M.P.) – 482001, India mnlbpi{at}rediffmail.com

Sutanjay Saxena

Seema Dubey

Polymer Research Laboratory, Department of Chemistry, Government Model Science College (Autonomous), Jabalpur (M.P.) – 482001, India

The -amylase induced enzymatic degradation of terpolymeric beads, composed of calcium alginate, starch and poly(ethylene) glycol, were studied for gastrointestinal drug delivery. The beads demonstrated faster degradation with increased enzyme activity in the range 0.64 to 2.24IU/mL. A linear relationship of the degradation rates and corresponding enzyme concentration indicate that degradation is governed by Michaelis-Menten kinetics. The degradation rate was enhanced with increases in starch content in the beads. The smaller value of KM (3.15 x 10^–5 mol^–1 dm^–3) indicated higher enzyme-substrate affinity. The beads crosslinked with barium ions demonstrated slower degradation due to a higher degree of crosslinking in the beads. With increases in initial water content, the degradation was found to increase. In order to incorporate in vivo GI conditions, the degradation was also studied using a flow through diffusion cell (FTDC). The hydrogel beads exhibited slower degradation by FTDC compared to traditional in vitro methods and the degradation was dependent on the nature of the filler particles used in the diffusion cell.

Key Words: enzyme degradation • polymeric beads • gastrointestinal drug delivery amylase • sodium alginate • beads • flow through diffusion cell • FTDC

Journal of Bioactive and Compatible Polymers, Vol. 21, No. 3, 237-255 (2006)
DOI: 10.1177/0883911506064370


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