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Effect of paracellular permeation enhancers on intestinal permeability of two peptide drugs,enalaprilat and hexarelin, in rats

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Acta Pharmaceutica Sinica B 2021年第6期11卷 1667-1675页

作者： David Dahlgren Tobias Olander Markus Sjoblom Mikael Hedeland Hans Lennernas Department of Pharmaceutical Biosciences Translational Drug Discovery and DevelopmentUppsala UniversityUppsala 75236Sweden Department of Neuroscience Division of PhysiologyUppsala UniversityUppsala 75236Sweden Department of Medicinal Chemistry Analytical Pharmaceutical ChemistryUppsala UniversityUppsala 75236Sweden Department of Chemistry Environment and Feed HygieneNational Veterinary Institute(SVA)Uppsala 75189Sweden

Transcellular permeation enhancers are known to increase the intestinal permeability of enalaprilat,a 349 Da peptide,but not hexarelin(887 Da).The primary aim of this paper was to investigate if paracellular permeability enhancers affected the intestinal permeation of the two *** was investigated using the rat single-pass intestinal perfusion model with concomitant blood *** luminal compositions included two paracellular permeation enhancers,chitosan(5 mg/mL) and ethylenediaminetetraacetate(EDTA,1 and 5 mg/mL),as well as low luminal tonicity(100 mOsm) with or without *** were evaluated by the change in lumen-to-blood permeability of hexarelin and enalaprilat,and the blood-to-lumen clearance of ^(51)chromium-labeled EDTA(CL_(Cr-EDTA)),a clinical marker for mucosal barrier *** two paracellular permeation enhancers increased the mucosal permeability of both peptide drugs to a similar *** data in this study suggests that the potential for paracellular permeability enhancers to increase intestinal absorption of hydrophilic peptides with low molecular mass is greater than for those with transcellular ***,the mucosal blood-to-lumen flux of ^(51)Cr-EDTA was increased by the two paracellular permeation enhancers and by luminal *** contrast,luminal hypotonicity did not affect the lumen-to-blood transport of enalaprilat and *** suggests that hypotonicity affects paracellular solute transport primarily in the mucosal crypt region,as this area is protected from luminal contents by a constant water flow from the crypts.

关键词： Permeation enhancers Absorption-modifying excipients Oral peptide delivery intestinal permeability intestinal perfusion Pharmaceutical development

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