Sustained gastrointestinal activity of dendronized polymer–enzyme conjugates View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2013-07

AUTHORS

Gregor Fuhrmann, Andrea Grotzky, Ružica Lukić, Simon Matoori, Paola Luciani, Hao Yu, Baozhong Zhang, Peter Walde, A. Dieter Schlüter, Marc A. Gauthier, Jean-Christophe Leroux

ABSTRACT

Methods to stabilize and retain enzyme activity in the gastrointestinal tract are investigated rarely because of the difficulty of protecting proteins from an environment that has evolved to promote their digestion. Preventing the degradation of enzymes under these conditions, however, is critical for the development of new protein-based oral therapies. Here we show that covalent conjugation to polymers can stabilize orally administered therapeutic enzymes at different locations in the gastrointestinal tract. Architecturally and functionally diverse polymers are used to protect enzymes sterically from inactivation and to promote interactions with mucin on the stomach wall. Using this approach the in vivo activity of enzymes can be sustained for several hours in the stomach and/or in the small intestine. These findings provide new insight and a firm basis for the development of new therapeutic and imaging strategies based on orally administered proteins using a simple and accessible technology. More... »

PAGES

582-589

Identifiers

URI

http://scigraph.springernature.com/pub.10.1038/nchem.1675

DOI

http://dx.doi.org/10.1038/nchem.1675

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1026635738

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/23787748


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