ENZYMATIC CLEAVAGE OF DISACCHARIDE SIDE-GROUPS IN INSOLUBLE SYNTHETIC-POLYMERS - A NEW METHOD FOR SPECIFIC DELIVERY OF DRUGS TO THE COLON

A series of water-insoluble acrylic polymers containing disaccharide s ide groups were synthesized and evaluated in vitro. A cellobiose-deriv ed monomer, lucopyranosyl-1-methacrylamido-1-deoxy-D-glucitol, was pre pared and copolymerized with methacrylic acid. Two different modes of polymerization were used to give two products, P-1 and P-2. A homopoly mer, P-3, was also synthesized using the same method as P-2. The degra dation of the disaccharide side groups in these polymers and the monom er was evaluated by incubation with beta-glucosidase and measurement o f the amount of glucose cleaved. It was found that the degradation rat e increased in those polymers possessing lower contents of the disacch aride side groups (i.e. higher content of methacrylic acid). Scanning electron microscopy (SEM) observations of cross-sectioned slabs of P-1 visualized the degradation of the polymer. The enzymatic reaction cau sed a porous structure to be formed. The increased porosity may be use d for the specific release of drugs into organs that contain large amo unts of beta-glucosidases, such as the human colon.