Search results for "Intestinal Absorption"
showing 10 items of 179 documents
Indicaxanthin inhibits NADPH oxidase (NOX)-1 activation and NF-κB-dependent release of inflammatory mediators and prevents the increase of epithelial…
2014
Dietary redox-active/antioxidant phytochemicals may help control or mitigate the inflammatory response in chronic inflammatory bowel disease (IBD). In the present study, the anti-inflammatory activity of indicaxanthin (Ind), a pigment from the edible fruit of cactus pear (Opuntia ficus-indica, L.), was shown in an IBD model consisting of a human intestinal epithelial cell line (Caco-2 cells) stimulated by IL-1β, a cytokine known to play a major role in the initiation and amplification of inflammatory activity in IBD. The exposure of Caco-2 cells to IL-1β brought about the activation of NADPH oxidase (NOX-1) and the generation of reactive oxygen species (ROS) to activate intracellular signal…
An approach to As(III) and As(V) bioavailability studies with Caco-2 cells
2005
Foods and drinking water are the main sources of human exposure to inorganic arsenic [As(III) and As(V)]. After oral ingestion, the intestinal epithelium is the first barrier to absorption of these species. A human intestinal cell line (Caco-2) was used to evaluate cell retention and transport of As(III) (15.6-156.0 microM) and/or As(V) (15.4-170.6 microM). Cell monolayer integrity, cell viability, membrane damage and effects on cell metabolism were evaluated. Only the highest concentrations assayed [As(III): 156.0 microM; As(V): 170.6 microM] produced a cytotoxic effect with different cellular targets: As(III) altered the permeability of tight junctions, and As(V) caused uncoupling of the …
Vitamin E transport, membrane incorporation and cell metabolism: Is α-tocopherol in lipid rafts an oar in the lifeboat?
2010
International audience; Vitamin E is composed of closely related compounds, including tocopherols and tocotrienols. Studies of the last decade provide strong support for a specific role of alpha-tocopherol in cell signalling and the regulation of gene expression. It produces significant effects on inflammation, cell proliferation and apoptosis that are not shared by other vitamin E isomers with similar antioxidant properties. The different behaviours of vitamin E isomers might relate, at least in part, to the specific effects they exert at the plasma membrane. alpha-Tocopherol is not randomly distributed throughout the phospholipid bilayer of biological membranes, and as compared with other…
Activity–Bioavailability balance in Oral Drug Development for a Selected Group of 6‐Fluoroquinolones
2002
Abstract A nomogram is proposed to select the best candidate in drug development studies with quinolones and is intended to substitute other possible models. The nomogram is referred to as an activity–bioavailability balance (ABB) because it includes the following two criteria: ABB= 1 / gm MIC ( drug candidate ) 1 /gm MIC ( ciprofloxacin ) · F calc \( drug candidate \) F calc ( ciproflaxacin ) . The in vitro activity of a group of 4′ N ‐alkyl‐ciprofloxacin derivatives was determined together with that of ciprofloxacin, initially against some reference strains and subsequently against 159 clinical isolates of eight selected species. The inverse of the geometric mean of the lowest concentrati…
Zur Frage der Resorption von Polyphosphaten
1965
Zur Klarung der Frage nach der Resorption von Polyphosphaten wurden Losungen von32P-markiertem Diphosphat, Triphosphat und einem Natriumpolyphosphat mit 64% P2O5 Ratten mit der Schlundsonde appliziert. Nach einer Verweildauer von 1, 2, 4, 8 und 16 Std dieser Polyphosphate im Magen-Darmtrakt wurden die Ratten dekapitiert und das erhaltene Frischblut radiometrisch und papierchromatographisch untersucht. Im enteiweisten Vollblut konnten nur Monophosphat und AMP nachgewiesen werden, d. h. es wird ausschlieslich anorganisches Monophosphat resorbiert, das durch enzymatische Aufspaltung der Polyphosphate gebildet wird. Dieses Monophosphat wird dann in die organische Bindung der AMP ubergefuhrt und…
Intestinal absorption enhancement via the paracellular route by fatty acids, chitosans and others: a target for drug delivery.
2005
Peroral delivery of hydrophilic drugs is one of the greatest challenges in biopharmaceutical research. Hydrophilic drugs usually present low bioavailability after oral administration. One of the causes of this low bioavailability is their poor intestinal permeation through the paracellular pathway. This pathway is actually restricted by the presence of tight junctions at the apical side of the enterocytes. In the last few years, great interest has been focused on the structure and cellular regulation of tight junctions, materializing in more in-depth knowledge of this intestinal barrier. Simultaneously, and on the basis of this understanding, continuous efforts are being made to develop age…
Compared effects of synthetic and natural bile acid surfactant on xenobiotic absorption. II. Studies with sodium glycocholate to confirm a hypothesis
1994
Abstract The effects of sodium glycocholate (SGC) on the intestinal absorption of drug-related xeriobiotics are investigated, on the basis of previously established absorption/partition relationships. Six phenylalkylcarboxylic acids, closely related to nonsteroid anti-inflammatory drugs in structure and constituting a true homologous series, were used as test compounds through an in situ rat gut technique, using the whole colon as nonspecialized absorption membrane model. Whereas the synthetic surfactants (i.e., polysorbates and laurylsulphates) at the critical micelle concentration have been shown to disrupt the aqueous boundary layer adjacent to the membrane, SGC does not; in contrast, it…
Effects of polysorbate 80 on amiodarone intestinal absorption in the rat
1995
Abstract Amiodarone is a widely used anti-arrhythmic agent which shows physico-chemical properties that are highly suitable for diffusion across lipophilic absorbing membranes, however,.its low aqueous solubility could represent the rate-limiting step for absorption, making it erratic and variable. In a previous paper, the influence of an anionic surfactant (sodium lauryl sulphate) at variable supramicellar concentrations was studied. The absorption rate constants of amiodarone decreased as the surfactant concentration increased, and absorption was unusually fast at lower surfactant concentrations. The previously proposed equations for interpreting the relationships between the amiodarone a…
Digestive disorders and Intestinal microbiota
2018
In the last decade, a barge body of scientific literature has suggested that specific alterations of the gut microbiota may be associated with ther development and clinical course of several gastrointestinal diseases, including irritable bowel syndrome, inflammatory bowel disease, celiac disease, gastrointestinal cancer and Clostridium difficile infection. These alterations are often referred to as “dysbiosis”, a generic term designing reduction of gut microbiota biodiversity and alterations in its composition. Here, we provide a synthetic overview of the key concepts on the relationship between intestinal microbiota and gastrointestinal diseases, focusing on the translation of these concep…
Preclinical models for colonic absorption, application to controlled release formulation development.
2018
Oral controlled release (CR) formulations have many benefits and have become a valuable resource for the local and systemic administration of drugs. The most important characteristic of these pharmaceutical products is that drug absorption occurs mainly in the colon. Therefore, this review analyses the physiological and physicochemical features that may affect an orally administered CR product, as well as the different strategies to develop a CR dosage form and the methods used to evaluate the formulation efficacy. The models available to study the intestinal permeability and their applicability to colonic permeability determinations are also discussed.