Curcumin has been traditionally used in food recipes for biological health benefits. However, these properties are compromised due to its very low bioavailability. Thus, this work assessed the impact of using natural potential bioenhancers improve intestinal permeability and understanding interaction flavonoids with curcuminoids through molecular dynamic simulation. The (Papp) was measured on h...

BACKGROUND Irritable bowel syndrome (IBS) is a disorder with multifactorial pathophysiology. Intestinal barrier may be altered, especially in diarrhea-predominant IBS (IBS-D). Several mediators may contribute to increased intestinal permeability in IBS. AIM We aimed to assess effects of tryptase and LPS on in vitro permeability using a 3-dimensional cell model after basolateral cell exposure....

A human small intestinal epithelial cell (HIEC) monolayer was recently established in our laboratories as a novel system to evaluate the Papp (apparent permeability coefficient) of compounds during their absorption in humans. An effusion-based analysis using polyethylene glycol oligomers with molecular weights ranging from 194-898 indicated that HIEC and Caco-2 cell monolayers both had paracell...

21 Acetyl salicylic acid (ASA) is one of the most frequently prescribed 22 medications for the secondary prevention of cardiovascular and cerebrovascular events. 23 It has recently been reported to cause small intestinal mucosal injury at a considerably 24 higher rate than previously believed. The aim of this study is to investigate the 25 mechanism by which this occurs using an in vitro small ...

Interleukin-1β (IL-1β) is a prototypical multifunctional cytokine that plays an important role in intestinal inflammation of Crohn's disease and other inflammatory conditions of the gut. Previous studies have shown that IL-1β causes an increase in intestinal epithelial tight junction (TJ) permeability both in in vivo animal and in vitro cell culture model systems. The IL-1β-induced increase in ...

objective(s):transporters have an important role in pharmacokinetics of drugs. inhibition or induction of drug transporters activity can affect drug absorption, safety, and efficacy. p-glycoprotein (p-gp) is the most important membrane transporter that is responsible for active efflux of drugs. it is important to understand which drugs are substrates, inhibitors, or inducers of p-gp to minimize...

BACKGROUND/AIMS Acetaminophen (APAP) effects on intestinal barrier properties are less investigated. APAP may lead to a changed bioavailability of a subsequently administered drug or diet in the body. We investigated the influence of APAP on enterocytic cell membrane properties that are able to modify the net intestinal absorption of administered substances across the Caco-2 barrier model. ME...

Invasion in and translocation across enterocytes are major events during Campylobacter jejuni-induced enteritis in humans. C. jejuni in vitro infection of cell monolayers typically results in loss of tight junction integrity, which could contribute to translocation. In the present study, we wanted to investigate whether butyrate is able to confer protection to Caco-2 cells against C. jejuni inv...

Preclinical prediction of intestinal drug absorption is a continuous challenge in drug development. The absorption of a drug from the gastrointestinal tract is a complicated process, involving passive membrane permeability parameters as well as many active transport and metabolism components. Therefore, well characterised and reliable in vitro methods for studying drug absorption are constantly...

We bring together fifteen, nonredundant, tabulated collections (amounting to 696 separate measurements) of the apparent permeability (P app) of Caco-2 cells to marketed drugs. While in some cases there are some significant interlaboratory disparities, most are quite minor. Most drugs are not especially permeable through Caco-2 cells, with the median P app value being some 16 ⋅ 10(-6) cm s(-1). ...