Search results for "Permeability"
showing 10 items of 596 documents
Modulation of drug transport by selected flavonoids: Involvement of P-gp and OCT?
2004
Flavonoids, as a common component of daily nutrition, are a possible source of interference with absorption processes, due to modulation of transporting proteins. In this study, the influence of selected flavonoids (quercetin, isoquercitrin, spiraeoside, rutin, kaempferol, naringenin, naringin, and kaempferol) on the transport of the P-gp substrate [3H]talinolol across Caco-2 cell monolayers was investigated. To elucidate the mechanism behind the interaction observed in this system the potency of the flavonoids to replace [3H]talinolol from its P-gp binding site as well as their activity to inhibit OCT2-mediated [14C]TEA uptake into LLC-PK(1) cells were measured, as P-gp and OCT have been s…
Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Ondansetron.
2019
Literature data pertaining to the physicochemical, pharmaceutical, and pharmacokinetic properties of ondansetron hydrochloride dihydrate are reviewed to arrive at a decision on whether a marketing authorization of an immediate release (IR) solid oral dosage form can be approved based on a Biopharmaceutics Classification System (BCS)-based biowaiver. Ondansetron, a 5HT3 receptor antagonist, is used at doses ranging from 4 mg to 24 mg in the management of nausea and vomiting associated with chemotherapy, radiotherapy, and postoperative treatment. It is a weak base and thus exhibits pH-dependent solubility. However, it is able to meet the criteria of "high solubility" as well as "high permeabi…
Permeability of the bladder mucosa to thiotepa, adriamycin, and daunomycin in men and rabbits.
1976
The permeability of the bladder mucosa to thiotepa and to the anthraquinonic antibiotics, adriamycin and daunomycin, was investigated both in humans and in experimental animals. Instillations in rabbits were performed either in intact males or in animals with ligated ureters. Absorption of thiotepa was significantly higher than that of the antibiotics both in men and in rabbits. Furthermore, a qualitative difference was observed in rabbits in relation to time and with regard to fixation to vesical tissues. In man, absorption was highest after transurethral surgery. It was also increased in cases with extensive anaplastic tumours or in the presence of acute inflammatory reactions.
Inflammation is an amplifier of lung congestion by high lv filling pressure in hemodialysis patients: a longitudinal study
2019
Introduction Since infammation alters vascular permeability, including vascular permeability in the lung, we hypothesized that it can be an amplifer of lung congestion in a category of patients at high risk for pulmonary oedema like end stage kidney disease (ESKD) patients. Objective and methods We investigated the efect modifcation by systemic infammation (serum CRP) on the relationship between a surrogate of the flling pressure of the LV [left atrial volume indexed to the body surface area (LAVI)] and lung water in a series of 220 ESKD patients. Lung water was quantifed by the number of ultrasound B lines (US-B) on lung US. Six-hundred and three recordings were performed during a 2-year f…
Oxygen permeability of hydrogel contact lenses with organosilicon moieties
2002
Oxygen transport through two extended wear (day and night) hydrogel contact lenses that contain organosilicon moieties (balafilcon A and lotrafilcon A) was studied in the hydrate (hydrogel) and dry (xerogel) states. The water uptake increased the oxygen permeability [(Dk)app] and transmissibility [Dk/L(av)] coefficients of the dry materials by about 70%. The (Dk)app for the hydrated lenses was determined following the so-called stack procedure. The values obtained were 107 +/- 4 barrer for balafilcon A and 141 +/- 5 barrer for lotrafilcon A, about 5-10 times larger than those previously reported for conventional (without organosilicon moieties) extended wear hydrogels contact lenses. The Dk…
A promising camptothecin derivative: Semisynthesis, antitumor activity and intestinal permeability.
2014
Oral administration of camptothecin (Cm) derivatives and other antitumoral agents is being actively developed in order to improve the quality of life of patients with cancer. Though several lipophilic derivatives of CPT have shown interesting oral bioavailability in preclinical and clinical studies, only Topotecan has been approved for this route of administration. Semisynthesis, antitumor activity, biological inhibition mechanism, and in situ intestinal permeability of 9, 10-[1,3]-Dioxinocamptothecin (CDiox), an unexplored CPT derivative, have been studied in this paper. The hexacyclic analog was as effective as Topotecan and CPT in different tumor cell lines, showing an expected similar a…
Nature of sterols affects plasma membrane behavior and yeast survival during dehydration.
2011
International audience; The plasma membrane (PM) is a main site of injury during osmotic perturbation. Sterols, major lipids of the PM structure in eukaryotes, are thought to play a role in ensuring the stability of the lipid bilayer during physicochemical perturbations. Here, we investigated the relationship between the nature of PM sterols and resistance of the yeast Saccharomyces cerevisiae to hyperosmotic treatment. We compared the responses to osmotic dehydration (viability, sterol quantification, ultrastructure, cell volume, and membrane permeability) in the wild-type (WT) strain and the ergosterol mutant erg6Δ strain. Our main results suggest that the nature of membrane sterols gover…
Insight into the primary mode of action of TiO2 nanoparticles on Escherichia coli in the dark.
2015
16 pages; International audience; Large-scale production and incorporation of titanium dioxide nanoparticles (NP-TiO2 ) in consumer products leads to their potential release into the environment and raises the question of their toxicity. The bactericidal mechanism of NP-TiO2 under UV light is known to involve oxidative stress due to the generation of reactive oxygen species. In the dark, several studies revealed that NP-TiO2 can exert toxicological effects. However, the mode of action of these nanoparticles is still controversial. In the present study, we used a combination of fluorescent probes to show that NP-TiO2 causes Escherichia coli membrane depolarization and loss of integrity, lead…
Six years of progress in the oral biopharmaceutics area - A summary from the IMI OrBiTo project.
2020
OrBiTo was a precompetitive collaboration focused on the development of the next generation of Oral Biopharmaceutics Tools. The consortium included world leading scientists from nine universities, one regulatory agency, one non-profit research organisation, three small/medium sized specialist technology companies together with thirteen pharmaceutical companies. The goal of the OrBiTo project was to deliver a framework for rational application of predictive biopharmaceutics tools for oral drug delivery. This goal was achieved through novel prospective investigations to define new methodologies or refinement of existing tools. Extensive validation has been performed of novel and existing biop…
Tracer aroma compound transfer from a solid and complex-flavored food matrix packed in treated papers or plastic packaging film.
2007
The objective of this work was to study the transfer of four aroma compounds (ethyl butyrate, ethyl hexanoate, cis-3-hexenol, and benzaldehyde) from a solid and complex-flavored food matrix (sponge cake) toward and through packaging films placed in indirect contact during storage in accelerated aging conditions (38 °C and 86% relative humidity gradient). The efficiency of treated papers relative to that of standard paper and plastic as barrier was tested. Before storage, aroma compound volatility in the sponge cake was measured, and similar values were found between aroma compounds, due to the fat content of the sponge cake. Whatever the aroma compound, permeability values during storage we…