The uptake and transport of 9-nitrocamptothecin (9-NC), a potent anticancer agent, across Caco-2 cell monolayers was studied as a free and PLGA nanoparticle loaded drug. Different sizes (110 to 950 nm) of 9-nitrocamptothecin nanoparticles using poly (lactic-glycolic acid) were prepared by via the nanoprecipitation method. The transport of nanoparticles across the Caco-2 cell monolayer as a func...

This study aimed to determine whether the fat and protein content in dairy-fruit blends prepared using full-fat, semi-skimmed, skimmed or high-protein milk combination with freeze-dried blackberry puree influenced bioaccessibility bioavailability of polyphenols organic acids. Samples were subjected vitro digestion, after which was analysed a Caco-2 cell model. The addition resulted formation ag...

Oligopeptides are generally thought to have poor permeability across biological membranes. Recent studies, however, suggest significant distribution of [Dmt1]DALDA (Dmt-D-Arg-Phe-Lys-NH2; Dmt is 2',6'-dimethyltyrosine), a 3+ net charge opioid peptide, to the brain and spinal cord after subcutaneous administration. Peptide transporters (PEPT1 and PEPT2) play a major role in the uptake of di- and...

Purpose: Quantitative Structure–Permeability Relationships (QSPerR) of the intestinal permeability across the (Caco-2) cells monolayer could be obtained by the application of new molecular descriptors. Method: A novel topologic-molecular approach to computer molecular design (TOMOCOMDCARDD) has been used to estimate the intestinal-epithelial transport of drug in Caco-2 cell culture. Results: Th...

BACKGROUND N-alkylamides (NAAs) are a large group of secondary metabolites occurring in more than 25 plant families which are often used in traditional medicine. A prominent active NAA is spilanthol. The general goal was to quantitatively investigate the gut mucosa and blood-brain barrier (BBB) permeability pharmacokinetic properties of spilanthol. METHODS Spilanthes acmella (L.) L. extracts,...

Epithelial barrier dysfunction has been implicated as one of the major contributors to the pathogenesis of inflammatory bowel disease. The increase in intestinal permeability allows the translocation of luminal antigens across the intestinal epithelium, leading to the exacerbation of colitis. Thus, therapies targeted at specifically restoring tight junction barrier function are thought to have ...

BACKGROUND The mucosal tissues play a central role in the transmission of HIV-1 infection as well as in the pathogenesis of AIDS. Despite several clinical studies reported intestinal dysfunction during HIV infection, the mechanisms underlying HIV-induced impairments of mucosal epithelial barrier are still unclear. It has been postulated that HIV-1 alters enterocytic function and HIV-1 proteins ...

Intestinal cells are the first line of defense against toxic substances that may enter the body orally. Some of these substances may emanate from wastewater treatment plants and thus may eventually enter the food chain. In this study, human intestinal Caco-2 cells were incubated with biologically treated activated sludge and lipopolysaccharide (LPS) to determine changes in protein expression an...

Solid drug nanoparticles (SDNs) are a nanotechnology with favourable characteristics to enhance drug delivery and improve the treatment of several diseases, showing benefit for improved oral bioavailability and injectable long-acting medicines. The physicochemical properties and composition of nanoformulations can influence the absorption, distribution, and elimination of nanoparticles; consequ...