Enzyme inhibition mucoadhesive polymers

Mucoadhesive polymers exhibiting strong complexing properties are capable of inhibiting intestinal brush border membrane-bound proteases through a far distance inhibitory effect [65]. In vivo, the mucoadhesive polymer is separated from the brush border membrane by a mucus layer [30]. Although there is no direct contact between polymer- and membrane-bound enzymes, it could be shown that inhibition takes place. The exploitation of this far distance effect seems to be a very promising alternative to small molecular mass inhibitors, which are currently used as inhibitors of brush border membrane-bound proteases. 

In a recent study, some authors proposed the employment of thiolated polymers obtained by the immobilization of thiol groups on well-established multifunctional polymers such as poly(acrylates) and chitosans as functional agents having mucoadhesive, penetration enhancement, and enzyme-inhibiting properties [94,95]. 

Recent studies have shown that in addition to their mucoadhesive effects, these polymers can also enhance oral bioavailability by inhibiting enzymes which deactivate the dmg moiety in the GI tract. Both... 

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