Mucoadhesive polymers in peroral peptide drug delivery. IV. Polycarbophil and chitosan are potent enhancers of peptide transport across intestinal mucosae in vitro

摘要: Abstract The purpose of the study was to evaluate inhibitory effect mucoadhesive polymers polycarbophil, chitosan and glutamate on trypsin carboxypeptidase B (CPB) activity as well their potential improve intestinal transport peptide drug 9-desglycinamide, 8- l -arginine vasopressin (DGAVP) in vitro. degradation model substrates N-α-benzoyl- ethylester by hippuryl- CPB presence studied. Furthermore, DGAVP investigated using Caco-2 cell monolayers rat vertically perfused loop model. Uniquely, polycarbophil a concentration 1% (w/v) able inhibit both activities. Chitosan concentrations 0.4 strongly increased across monolayers, whereas showed only low enhancement. All (w/v), however, pronounced comparable improvement mucosae It is concluded that chitosans enhance solely increasing paracellular permeability due opening intercellular junctions. observed mainly ascribed protection against proteolytic lumen, which allows for sufficient thus when induced less enhanced.