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Stabilization of enzymes with polycationic branched polymers

Stabilization of enzymes with polycationic branched polymers could improve the oral delivery of therapeutics. Poly-(3,5-bis(3-aminopropoxy)benzyl)-methacrylate was conjugated to a bacteria-derived, proline-specific endopeptidase. In rats, the endopeptidase-polymer conjugate showed greater retention and catalytic activity within the stomach than the same enzyme conjugated to polymers that stabilize proteins for systemic delivery. Next steps include evaluating the impact of polymer structure, molecular weight and conjugation site on efficacy and safety.

SciBX 6(27); doi:10.1038/scibx.2013.707
Published online July 18, 2013

Unpatented; licensing status not applicable

Fuhrmann, G. et al. Nat. Chem.; published online June 9, 2013;
doi:10.1038/nchem.1675
Contact: Jean-Christophe Leroux, Swiss Federal Institute of Technology Zurich (ETHZ), Zurich, Switzerland
e-mail:

jleroux@ethz.ch