Permeability-enhancing effects of three laurate-disaccharide monoesters across isolated rat intestinal mucosae

Laurate (C 12 )-sucrose esters are established intestinal epithelial permeation enhancers (PEs) with potential for use in oral delivery. Most studies have examined blends of ester rather than specific monoesters, little variation on the sugar moiety. To investigate influence varying moiety monoester performance, we compared three monoesters: C -sucrose, -lactose, and -trehalose. The assays were: critical micellar concentration (CMC) Krebs-Henseleit buffer, MTS lactate dehydrogenase Caco-2 cells, transepithelial electrical resistance (TEER) apparent permeability coefficient (P app ) [ 14 C] mannitol across isolated rat mucosae, tissue histology. For CMC, rank order was -trehalose (0.21 mM) < -sucrose (0.34 -lactose (0.43 mM). Exposure to cells 120 min produced TC 50 values assay from 0.1 0.4 mM. Each a concentration-dependent decrease TEER mucosae 80% reduction seen 8 mM 5 min, but less potent. increased P similar potency efficacy, whereas not as potent or efficacious, even though it still flux. In presence esters, gross histology unaffected except at -lactose. conclusion, enhanced likely via tight junction modulation tissue. quite neither did damage same extent. All can be considered PEs included formulations.