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https://www.readbyqxmd.com/read/27914234/food-gastrointestinal-ph-and-models-of-oral-drug-absorption
#1
REVIEW
Ahmad Y Abuhelwa, Desmond B Williams, Richard N Upton, David J R Foster
This article reviews the major physiological and physicochemical principles of the effect of food and gastrointestinal (GI) pH on the absorption and bioavailability of oral drugs, and the various absorption models that are used to describe/predict oral drug absorption. The rate and extent of oral drug absorption is determined by a complex interaction between a drug's physicochemical properties, GI physiologic factors, and the nature of the formulation administered. GI pH is an important factor that can markedly affect oral drug absorption and bioavailability as it may have significant influence on drug dissolution & solubility, drug release, drug stability, and intestinal permeability...
November 30, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27914041/paliperidone-loaded-nanolipomer-system-for-sustained-delivery-and-enhanced-intestinal-permeation-superiority-to-polymeric-and-solid-lipid-nanoparticles
#2
Hala Mahmoud Helal, Sana Mohamed Mortada, Marwa Ahmed Sallam
Paliperidone (PPD) is the most recent second-generation atypical antipsychotic approved for the treatment of schizophrenia. An immediate release dose causes extrapyramidal side effects. In this work, a novel nanolipomer carrier system for PPD with enhanced intestinal permeability and sustained release properties has been developed and optimized. PPD was successfully encapsulated into a lipomer consisting of a specific combination of biocompatible materials including poly-ε-caprolactone as a polymeric core, Lipoid S75, and Gelucire® 50/13 as a lipid shell and polyvinyl alcohol as a stabilizing agent...
December 2, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27912750/fermented-barley-and-soybean-bs-mixture-enhances-intestinal-barrier-function-in-dextran-sulfate-sodium-dss-induced-colitis-mouse-model
#3
Jong Kyu Woo, Seungho Choi, Ju-Hee Kang, Dae Eung Kim, Byung-Serk Hurh, Jong-Eun Jeon, Sun Yeou Kim, Seung Hyun Oh
BACKGROUND: Inflammatory bowel disease (IBD) is characterized by chronic or relapsing immune system activation and inflammation within the gastrointestinal tract. The lack of safety and efficacy of standard therapies, the use of food supplements for managing IBD is increasing, and many studies have reported that various food supplements provide many beneficial effects for the IBD. METHODS: This study aimed to evaluate the anti-colitis effects of dietary supplementation with a fermented barley and soybean mixture (BS) on intestinal inflammation using a murine model of IBD...
December 3, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27908847/homeostasis-of-the-gut-barrier-and-potential-biomarkers
#4
Jerry M Wells, Robert J Brummer, Muriel Derrien, Thomas T MacDonald, Freddy Troost, Patrice D Cani, Vassilia Theodorou, Jan Dekker, Agnes Méheust, Willem M de Vos, Annick Mercenier, Arjen Nauta, Clara L Garcia-Rodenas
The gut barrier plays a crucial role by spatially compartmentalizing bacteria to the lumen through the production of secreted mucus and is fortified by the production of sIgA and antimicrobial peptides and proteins. With exception of sIgA the expression of these protective barrier factors is largely controlled by innate immune recognition of microbial molecular ligands. Several specialized adaptations and checkpoints are operating in the mucosa to scale the immune response according to the threat and prevent overreaction to the trillions of symbionts inhabiting the human intestine...
December 1, 2016: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/27908629/evaluation-of-the-cytotoxicity-genotoxicity-and-mucus-permeation-capacity-of-several-surface-modified-poly-anhydride-nanoparticles-designed-for-oral-drug-delivery
#5
T Iglesias, A López de Cerain, Juan Manuel Irache, N Martín-Arbella, M Wilcox, J Pearson, A Azqueta
The main concerns with drugs designed for oral administration are their inactivation or degradation in the harsh conditions of the gastrointestinal tract, their poor solubility through the gastrointestinal mucus gel layer, the poor intestinal epithelium permeability that limits their absorption, and their toxicity. In this context, poly(anhydride) nanoparticles are capable of protecting the drug from the harsh environment, reduce the drug's toxicity and, by virtue of surface modification, to enhance or reduce their mucus permeability and the bioadhesion to specific target cells...
November 28, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27907206/intestinal-fluid-permeability-in-atlantic-salmon-salmo-salar-l-is-affected-by-dietary-protein-source
#6
Haibin Hu, Trond M Kortner, Karina Gajardo, Elvis Chikwati, John Tinsley, Åshild Krogdahl
In Atlantic salmon (Salmo salar L.), and also in other fish species, certain plant protein ingredients can increase fecal water content creating a diarrhea-like condition which may impair gut function and reduce fish growth. The present study aimed to strengthen understanding of the underlying mechanisms by observing effects of various alternative plant protein sources when replacing fish meal on expression of genes encoding proteins playing key roles in regulation of water transport across the mucosa of the distal intestine (DI)...
2016: PloS One
https://www.readbyqxmd.com/read/27906964/undernutrition-vitamin-a-and-iron-deficiency-are-associated-with-impaired-intestinal-mucosal-permeability-in-young-bangladeshi-children-assessed-by-lactulose-mannitol-test
#7
Md Iqbal Hossain, Rashidul Haque, Dinesh Mondal, Mustafa Mahfuz, Am Shamsir Ahmed, M Munirul Islam, Richard L Guerrant, William A Petri, Tahmeed Ahmed
BACKGROUND: Lactulose/mannitol (L:M) test has been used as a non-invasive marker of intestinal mucosal -integrity and -permeability (enteropathy). We investigated the association of enteropathy with anthropometrics, micronutrient- status, and morbidity in children. METHODS: The urine and blood samples were collected from 925 children aged 6-24 months residing in Mirpur slum of Dhaka, Bangladesh during November 2009 to April 2013. L:M test and micronutrient status were assessed in the laboratory of International Centre for Diarrhoeal Diseases Research, Bangladesh (icddr,b) following standard procedure...
2016: PloS One
https://www.readbyqxmd.com/read/27906617/evaluation-of-cellular-purine-transport-and-metabolism-in-the-caco-2-cell-using-comprehensive-high-performance-liquid-chromatography-method-for-analysis-of-purines
#8
T Fukuuchi, M Kobayashi, N Yamaoka, K Kaneko
Using Caco-2 cells and our previously developed high-performance liquid chromatography method for quantification of purine bases, nucleosides, and nucleotides, we evaluated cellular purine transport and uptake. The analytes were separated using YMC-Triart C18 column with gradient elution. We used Caco-2 cells as intestinal model cells and monitored purine transport across a monolayer for 2 h. The degree of change of purine concentrations in the permeate was very slight; however, it was possible to simultaneously determine these parameters for all purines because of our method's high sensitivity...
December 2016: Nucleosides, Nucleotides & Nucleic Acids
https://www.readbyqxmd.com/read/27906427/the-role-of-diet-on-gut-microbiota-composition
#9
S Bibbò, G Ianiro, V Giorgio, F Scaldaferri, L Masucci, A Gasbarrini, G Cammarota
Gut microbiota is characterized by an inter-individual variability due to genetic and environmental factors. Among the environmental ones, dietary habits play a key role in the modulation of gut microbiota composition. There are main differences between the intestinal microbiota of subjects fed with prevalent Western diet and that of subjects with a diet rich in fibers. Specific changes in the composition of gut microbiota have been demonstrated among subjects according to a different dietary intake. A particular diet may promote the growth of specific bacterial strains, driving hosts to a consequent alteration of fermentative metabolism, with a direct effect on intestinal pH, which can be responsible for the development of a pathogenic flora...
November 2016: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/27906073/gut-barrier-structure-mucosal-immunity-and-intestinal-microbiota-in-the-pathogenesis-and-treatment-of-hiv-infection
#10
REVIEW
Camilla Tincati, Daniel C Douek, Giulia Marchetti
Over the past 10 years, extensive work has been carried out in the field of microbial translocation in HIV infection, ranging from studies on its clinical significance to investigations on its pathogenic features. In the present work, we review the most recent findings on this phenomenon, focusing on the predictive role of microbial translocation in HIV-related morbidity and mortality, the mechanisms by which it arises and potential therapeutic approaches. From a clinical perspective, current work has shown that markers of microbial translocation may be useful in predicting clinical events in untreated HIV infection, while conflicting data exist on their role in cART-experienced subjects, possibly due to the inclusion of extremely varied patient populations in cohort studies...
April 11, 2016: AIDS Research and Therapy
https://www.readbyqxmd.com/read/27905575/protoporphyrin-ix-modified-chitosan-g-oligo-nipaam-polymeric-micelles-from-physical-stabilization-to-permeability-characterization-in-vitro
#11
Inbar Schlachet, Alejandro Sosnik
Two main hurdles persist towards the more extensive bench-to-bed side translation of non-parenteral polymeric micelles. The first pertains to their thermodynamically-driven disassembly under uncontrolled dilution conditions in the biological milieu and upon interaction with biomacromolecules (e.g., proteins). The second is related to the relatively poor understanding of the pathways by which polymeric micelles improve the bioavailability of the payload by mucosal routes (e.g., intestinal). In this work, a chitosan-g-oligo(N-isopropylacrylamide) (CS-g-oligo(NiPAAm)) copolymer was modified with non-cytotoxic amounts of protoporphyrin IX (PP), a planar molecule of amphiphilic character that undergoes self-aggregation in water by forming π-π stacked supramolecular structures, to induce micellization under disfavored conditions and to serve as a fluorescent tracer for the measurement of the micelle permeability across a model of the intestinal epithelium in vitro...
December 1, 2016: Biomaterials Science
https://www.readbyqxmd.com/read/27902414/modulation-of-intestinal-barrier-function-to-ameliorate-salmonella-infection-in-mice-by-oral-administration-of-fermented-milks-produced-with-lactobacillus-plantarum-mtcc-5690-a-probiotic-strain-of-indian-gut-origin
#12
Namita Rokana, Rajbir Singh, Rashmi Hogarehalli Mallappa, Virender Kumar Batish, Sunita Grover
Probiotic Lactobacillus plantarum MTCC 5690 -a probiotic strain of Indian gut origin as such and milk formulations produced with the same were explored in this sudy as biotherapeutics by evauating their functional efficacy against Salmonella infection in mice. The efficacy of milk formulations (fermented/unfermented) of MTCC 5690 for enhancement of intestinal barrier function was determined by monitoring the permeability and histopathology of intestine. The mice fed with probiotic Dahi (PD), Fermented Probiotic Drink (FD) and Sweetened fermented probiotic drink (SFD) maintained the health and integrity of intestinal epithelium in the infected mice as compared to those fed with phosphate buffered saline, milk, unfermented probiotic milk and Dahi...
October 17, 2016: Journal of Medical Microbiology
https://www.readbyqxmd.com/read/27901358/mdck-cells-are-capable-of-water-secretion-and-reabsorption-in-response-to-changes-in-the-ionic-environment
#13
Janne P Capra, Sinikka M Eskelinen
A prerequisite for tissue electrolyte homeostasis is highly regulated ion and water transport through kidney or intestinal epithelia. In the present work, we monitored changes in the cell and luminal volumes of type II Madin-Darby canine kidney (MDCK) cells grown in a 3D environment in response to drugs, or to changes in the composition of the basal extracellular fluid. Using fluorescent markers and high-resolution spinning disc confocal microscopy, we could show that lack of sodium and potassium ions in the basal fluid (tetramethylammonium chloride (TMACl) buffer) induces a rapid increase in the cell and luminal volumes...
September 1, 2016: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/27901175/adme-studies-and-preliminary-safety-pharmacology-of-ldt5-a-lead-compound-for-the-treatment-of-benign-prostatic-hyperplasia
#14
F Noël, J B Nascimento-Viana, L A S Romeiro, R O Silva, L F N Lemes, A S Oliveira, T B S Giorno, P D Fernandes, C L M Silva
This study aimed to estimate the absorption, distribution, metabolism and excretion (ADME) properties and safety of LDT5, a lead compound for oral treatment of benign prostatic hyperplasia that has previously been characterized as a multi-target antagonist of α1A-, α1D-adrenoceptors and 5-HT1A receptors. The preclinical characterization of this compound comprised the evaluation of its in vitro properties, including plasma, microsomal and hepatocytes stability, cytochrome P450 metabolism and inhibition, plasma protein binding, and permeability using MDCK-MDR1 cells...
2016: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/27900602/transepithelial-transport-of-curcumin-in-caco-2-cells-is-significantly-enhanced-by-micellar-solubilisation
#15
Jan Frank, Christina Schiborr, Alexa Kocher, Jürgen Meins, Dariush Behnam, Manfred Schubert-Zsilavecz, Mona Abdel-Tawab
Curcumin, the active constituent of Curcuma longa L. (family Zingiberaceae), has gained increasing interest because of its anti-cancer, anti-inflammatory, anti-diabetic, and anti-rheumatic properties associated with good tolerability and safety up to very high doses of 12 g. Nanoscaled micellar formulations on the base of Tween 80 represent a promising strategy to overcome its low oral bioavailability. We therefore aimed to investigate the uptake and transepithelial transport of native curcumin (CUR) vs. a nanoscaled micellar formulation (Sol-CUR) in a Caco-2 cell model...
November 29, 2016: Plant Foods for Human Nutrition
https://www.readbyqxmd.com/read/27898676/dietary-butyrate-helps-to-restore-the-intestinal-status-of-a-marine-teleost-sparus-aurata-fed-extreme-diets-low-in-fish-meal-and-fish-oil
#16
Itziar Estensoro, Gabriel Ballester-Lozano, Laura Benedito-Palos, Fabian Grammes, Juan Antonio Martos-Sitcha, Liv-Torunn Mydland, Josep Alvar Calduch-Giner, Juan Fuentes, Vasileios Karalazos, Álvaro Ortiz, Margareth Øverland, Ariadna Sitjà-Bobadilla, Jaume Pérez-Sánchez
There is a constant need to find feed additives that improve health and nutrition of farmed fish and lessen the intestinal inflammation induced by plant-based ingredients. The objective of this study was to evaluate the effects of adding an organic acid salt to alleviate some of the detrimental effects of extreme plant-ingredient substitution of fish meal (FM) and fish oil (FO) in gilthead sea bream diet. Three experiments were conducted. In a first trial (T1), the best dose (0.4%) of sodium butyrate (BP-70 ®NOREL) was chosen after a short (9-weeks) feeding period...
2016: PloS One
https://www.readbyqxmd.com/read/27895892/sexual-dimorphism-in-the-mast-cell-transcriptome-and-the-pathophysiological-responses-to-immunological-and-psychological-stress
#17
Emily Mackey, Saravanan Ayyadurai, Calvin S Pohl, Susan D' Costa, Yihang Li, Adam J Moeser
BACKGROUND: Biological sex plays a prominent role in the prevalence and severity of a number of important stress-related gastrointestinal and immune-related diseases including IBS and allergy/anaphylaxis. Despite the establishment of sex differences in these diseases, the underlying mechanisms contributing to sex differences remain poorly understood. The objective of this study was to define the role of biological sex on mast cells (MCs), an innate immune cell central to the pathophysiology of many GI and allergic disorders...
2016: Biology of Sex Differences
https://www.readbyqxmd.com/read/27895587/vitamin-d-signaling-through-induction-of-paneth-cell-defensins-maintains-gut-microbiota-and-improves-metabolic-disorders-and-hepatic-steatosis-in-animal-models
#18
Danmei Su, Yuanyang Nie, Airu Zhu, Zishuo Chen, Pengfei Wu, Li Zhang, Mei Luo, Qun Sun, Linbi Cai, Yuchen Lai, Zhixiong Xiao, Zhongping Duan, Sujun Zheng, Guihui Wu, Richard Hu, Hidekazu Tsukamoto, Aurelia Lugea, Zhenqui Liu, Stephen J Pandol, Yuan-Ping Han
Metabolic syndrome (MetS), characterized as obesity, insulin resistance, and non-alcoholic fatty liver diseases (NAFLD), is associated with vitamin D insufficiency/deficiency in epidemiological studies, while the underlying mechanism is poorly addressed. On the other hand, disorder of gut microbiota, namely dysbiosis, is known to cause MetS and NAFLD. It is also known that systemic inflammation blocks insulin signaling pathways, leading to insulin resistance and glucose intolerance, which are the driving force for hepatic steatosis...
2016: Frontiers in Physiology
https://www.readbyqxmd.com/read/27895415/factoring-the-intestinal-microbiome-into-the-pathogenesis-of-autoimmune-hepatitis
#19
EDITORIAL
Albert J Czaja
The intestinal microbiome is a reservoir of microbial antigens and activated immune cells. The aims of this review were to describe the role of the intestinal microbiome in generating innate and adaptive immune responses, indicate how these responses contribute to the development of systemic immune-mediated diseases, and encourage investigations that improve the understanding and management of autoimmune hepatitis. Alterations in the composition of the intestinal microflora (dysbiosis) can disrupt intestinal and systemic immune tolerances for commensal bacteria...
November 14, 2016: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/27891580/acute-infection-with-the-intestinal-parasite-trichuris-muris-has-long-term-consequences-on-mucosal-mast-cell-homeostasis-and-epithelial-integrity
#20
Daniel Sorobetea, Jacob Bak Holm, Henrietta Henningsson, Karsten Kristiansen, Marcus Svensson-Frej
A hallmark of parasite infection is the accumulation of innate immune cells, notably granulocytes and mast cells, at the site of infection. While this is typically viewed as a transient response, with the tissue returning to steady state once the infection is cleared, we found that mast cells accumulated in the large-intestinal epithelium following infection with the nematode Trichuris muris and persisted at this site for several months after worm expulsion. Mast cell accumulation in the epithelium was associated with the induction of type-2 immunity and appeared to be driven by increased maturation of local progenitors in the intestinal lamina propria...
November 28, 2016: European Journal of Immunology
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