Effects of absorption enhancers on cytoskeletal actin filaments in Caco-2 cell monolayers
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Mechanisms of white mustard seed (Sinapis alba L.) volatile oils as transdermal penetration enhancers
2019, FitoterapiaCitation Excerpt :Ionotropic glutamate receptors of the N -methyl- d -aspartate (NMDA) receptor type and transient receptor potential A1(TRPA1) could enable a transmembranous calcium influx from the extracellular space. Increased Ca2+ concentration in human keratinocytes can cause contraction of actin filaments and contraction of cells [22], increasing intercellular space and skin permeability, allowing drugs to penetrate the skin more easily. This study found that SVO can increase the Ca2+ concentration in HaCaT cells, which is beneficial to increase the skin permeability of model drugs.
Intestinal permeation enhancers for oral peptide delivery
2016, Advanced Drug Delivery ReviewsSodium caprate-induced increases in intestinal permeability and epithelial damage are prevented by misoprostol
2015, European Journal of Pharmaceutics and BiopharmaceuticsCitation Excerpt :Its high hydrophilic–lipophilic balance (HLB) is indicative of detergent- and solubilization capacity. A concentration of 8.5 mM caused a cascade of event in Caco-2 monolayers: increased membrane fluidity and perturbation, resulting in activation of phospholipase C [39], increased intracellular calcium [40], depolymerization of cytoskeletal F-actin [41], and activation of myosin light chain kinase [42]. While these can be viewed as non-specific events, the removal of the tight junction proteins tricellulin and claudin-5 suggests some specific actions [43,44].
Sodium caprate as an enhancer of macromolecule permeation across tricellular tight junctions of intestinal cells
2013, BiomaterialsCitation Excerpt :Previously, the effects of caprate have also been reported in the intestinal cell line Caco-2 [50], and MDCK cells. In Caco-2-cells, effects on barrier function were mainly attributed to mechanisms mediated via actin–myosin interactions, which were assumed to result in a retrieval of tight junction proteins from the apicolateral membrane [51,52]. However, this cell line only possesses low endogenous expression of (i) claudin-5, and (ii) tricellulin; the structural correlate for tricellular macromolecule permeability, has not been analyzed.
Enhanced oral absorption of paclitaxel in N-deoxycholic acid-N, O-hydroxyethyl chitosan micellar system
2010, Journal of Pharmaceutical SciencesCitation Excerpt :The significant differences in oral bioavailability between PTX-loaded DHC micelles and Taxol® were probably attributed to the following: Firstly, the constituents of DHC including hydroxyethyl chitosan and deoxycholic acid contributed to the absorption enhancement: (a) CS has mucoadhesive property, which is probably mediated through ionic interaction between positively charged amino groups in CS and negatively charged amino residues in mucus or on cell surfaces.21 Moreover, CS is able to interact with the tight junctions and to provoke their opening allowing for the entry of hydrophilic macromolecule;22 (b) deoxycholic acid is a kind of absorption enhancer, demonstrated to increase oral bioavailability via a combination of several postulated mechanisms, such as the alteration of biological membrane integrity, inhibition of proteases activity, or molecular aggregation through micellar solubilization.35,36 Secondly, the characteristic properties of micelles also played a key role here: (a) CMC value is the minimum concentration of a polymer that will result in micelle formation.