Quaternization of high molecular weight chitosan for increasing intestinal drug absorption using Caco-2 cells as an in vitro intestinal model.

ABSTRACT: Potential use of a quaternized chitosan (MW 600 kDa) with 65% of 3-chloro-2-hydroxypropyltrimethylammonium (600-HPTChC₆₅) as an absorptive enhancer was investigated in Caco-2 monolayers. 600-HPTChC₆₅ (0.005% w/v) quickly reduced transepithelial electrical resistance (TEER) to the maximum level in 40 min with full recovery within 6 h after removal. Its TEER reduction was corresponded to increased FD4 transport across the monolayers and disrupted localization of tight junction proteins ZO-1 and occludin at the cell borders. 600-HPTChC₆₅ was densely localized at the membrane surface and intercellular junctions. This chitosan (0.08-0.32% w/v) reduced the efflux ratio of [³H]-digoxin by 1.7- 2 folds, suggesting an increased [³H]-digoxin tra

SUBMITTER: Wongwanakul R 

PROVIDER: S-EPMC10188607 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature