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Intestinal permeability

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https://www.readbyqxmd.com/read/28540173/self-microemulsifying-drug-delivery-system-for-improving-the-bioavailability-of-huperzine-a-by-lymphatic-uptake
#1
Fang Li, Rongfeng Hu, Bin Wang, Yun Gui, Gang Cheng, Song Gao, Lei Ye, Jihui Tang
Huperzine A (Hup-A) is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion (SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration-time curve (AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension (P<0...
May 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28540164/understanding-peroral-absorption-regulatory-aspects-and-contemporary-approaches-to-tackling-solubility-and-permeability-hurdles
#2
REVIEW
Prachi B Shekhawat, Varsha B Pokharkar
Oral drug absorption is a process influenced by the physicochemical and biopharmaceutical properties of the drug and its inter-relationship with the gastrointestinal tract. Drug solubility, dissolution and permeability across intestinal barrier are the key parameters controlling absorption. This review provides an overview of the factors that affect drug absorption and the classification of a drug on the basis of solubility and permeability. The biopharmaceutical classification system (BCS) was introduced in early 90׳s and is a regulatory tool used to predict bioavailability problems associated with a new entity, thereby helping in the development of a drug product...
May 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28539338/expression-of-trans-and-paracellular-calcium-and-magnesium-transport-proteins-in-renal-and-intestinal-epithelia-during-lactation
#3
Megan R Beggs, Ida Appel, Per Svenningsen, Karsten Skjødt, R Todd Alexander, Henrik Dimke
Significant alterations in maternal calcium (Ca2+) and magnesium (Mg2+) balance occur during lactation. Ca2+ is the primary divalent cation mobilized into breast milk by demineralization of the skeleton and alterations in intestinal and renal Ca2+ transport. Mg2+ is also concentrated in breast milk, but the underlying mechanisms are not well understood. To determine the molecular alterations in Ca2+ and Mg2+ transport in the intestine and kidney during lactation, 3 groups of female mice consisting of either non-pregnant controls, lactating mice, or mice undergoing involution were examined...
May 24, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28539272/selenium-nanoparticles-as-versatile-carriers-for-oral-delivery-of-insulin-insight-into-the-synergic-antidiabetic-effect-and-mechanism
#4
Wenji Deng, Qian Xie, Huan Wang, Zhiguo Ma, Baojian Wu, Xingwang Zhang
Oral insulin delivery has been plagued by limited bioavailability. This work reports selenium nanoparticles (SeNPs) for oral insulin delivery to overcome the absorption barrier. Insulin-loaded SeNPs (INS-SeNPs) were fabricated by ionic cross-linking/in situ reduction and characterized by particle size and drug entrapment. The resultant INS-SeNPs were 120nm around in particle size with high drug loading. INS-SeNPs exhibited controllable insulin release and outstanding stability in the digestive fluids. INS-SeNPs caused a significant hypoglycemic effect in both normal and diabetic rats...
May 21, 2017: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/28537581/the-effects-of-a-multispecies-probiotic-on-migraine-and-markers-of-intestinal-permeability-results-of-a-randomized-placebo-controlled-study
#5
N M de Roos, S van Hemert, J M P Rovers, M G Smits, B J M Witteman
BACKGROUND/OBJECTIVES: Migraine, associated with several gastrointestinal disorders, may result from increased intestinal permeability, allowing endotoxins to enter the bloodstream. We tested whether probiotics could reduce migraine through an effect on intestinal permeability and inflammation. SUBJECTS/METHODS: In total, 63 patients were randomly allocated to the probiotic (n=31) or the placebo group (n=32). Participants ingested a multispecies probiotic (5x10(9) colony-forming units) or placebo daily for 12 weeks...
May 24, 2017: European Journal of Clinical Nutrition
https://www.readbyqxmd.com/read/28535336/transport-of-the-glucosamine-derived-browning-product-fructosazine-polyhydroxyalkylpyrazine-across-the-human-intestinal-caco-2-cell-monolayer-role-of-the-hexose-transporters
#6
Abhishek Bhattacherjee, Yuliya Hrynets, Mirko Betti
The transport mechanism of fructosazine, a glucosamine self-condensation product, was investigated using a Caco-2 cell model. Fructosazine transport was assessed by measuring the bidirectional permeability coefficient across Caco-2 cells. The mechanism of transport was evaluated using phlorizin, an inhibitor of sodium-dependent glucose cotransporters (SGLT) 1 and 2, phloretin and quercetin, an inhibitors of glucose transporters (GLUT) 1 and 2, transcytosis inhibitor wortmannin, and gap junction disruptor cytochalasin D...
May 23, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28534300/formulation-and-evaluation-of-naringenin-nanosuspensions-for-bioavailability-enhancement
#7
Sonia Gera, Sreekanth Talluri, Nagarjun Rangaraj, Sunitha Sampathi
The clinical potential of naringenin (NRG) is compromised due to its poor aqueous solubility and low oral bioavailability. The study is aimed at addressing these issues by means of naringenin nanosuspensions (NRG-NS) formulated using polyvinylpyrrolidone (PVP K-90) as stabiliser via antisolvent sonoprecipitation method. Optimisation of sonication time, drug concentration and stabilisers was done based on particle size. Characterisation of pure NRG and NRG-NS was carried out by scanning electron microscopy, differential scanning calorimetry (DSC), x-ray powder diffractometry (XRD) and Fourier transform infrared spectroscopy (FTIR)...
May 22, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28533908/ascites-refractory-ascites-and-hyponatremia-in-cirrhosis
#8
Brett Fortune, Andres Cardenas
Ascites is the most common complication related to cirrhosis and is associated with increased morbidity and mortality. Ascites is a consequence of the loss of compensatory mechanisms to maintain the overall effective arterial blood volume due to worsening splanchnic arterial vasodilation as a result of clinically significant portal hypertension. In order to maintain effective arterial blood volume, vasoconstrictor and antinatriuretic pathways are activated, which increase overall sodium and fluid retention...
May 2017: Gastroenterology Report
https://www.readbyqxmd.com/read/28533680/preparation-characterization-and-in-vitro-vivo-studies-of-oleanolic-acid-loaded-lactoferrin-nanoparticles
#9
Xiaojing Xia, Haowei Liu, Huixia Lv, Jing Zhang, Jianping Zhou, Zhiying Zhao
Oleanolic acid (OA), a pentacyclic triterpene, is used to safely and economically treat hepatopathy. However, OA, a Biopharmaceutics Classification System IV category drug, has low bioavailability owing to low solubility (<1 μg/mL) and biomembrane permeability. We developed a novel OA nanoparticle (OA-NP)-loaded lactoferrin (Lf) nanodelivery system with enhanced in vitro OA dissolution and improved oral absorption and bioavailability. The OA-NPs were prepared using NP albumin-bound technology and characterized using dynamic light scattering, scanning electron microscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro dissolution test...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28533127/primary-human-polarized-small-intestinal-epithelial-barriers-respond-differently-to-a-hazardous-and-an-innocuous-protein
#10
A D Eaton, C Zimmermann, B Delaney, B P Hurley
An experimental platform employing human derived intestinal epithelial cell (IEC) line monolayers grown on permeable Transwell(®) filters was previously investigated to differentiate between hazardous and innocuous proteins. This approach was effective at distinguishing these types of proteins and perturbation of monolayer integrity, particularly transepithelial electrical resistance (TEER), was the most sensitive indicator. In the current report, in vitro indicators of monolayer integrity, cytotoxicity, and inflammation were evaluated using primary (non-transformed) human polarized small intestinal epithelial barriers cultured on Transwell(®) filters to compare effects of a hazardous protein (Clostridium difficile Toxin A [ToxA]) and an innocuous protein (bovine serum albumin [BSA])...
May 19, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28528363/caffeic-acid-phenethyl-ester-is-protective-in-experimental-ulcerative-colitis-via-reduction-in-levels-of-pro-inflammatory-mediators-and-enhancement-of-epithelial-barrier-function
#11
Mohammed N Khan, Majella E Lane, Paul A McCarron, Murtaza M Tambuwala
BACKGROUND: Inhibition of the nuclear factor kappa beta (NF-κβ) pathway has been proposed as a therapeutic target due to its key role in the expression of pro-inflammatory genes, including pro-inflammatory cytokines, chemokines, and adhesion molecules. Caffeic acid phenethyl ester (CAPE) is a naturally occurring anti-inflammatory agent, found in propolis, and has been reported as a specific inhibitor of NF-κβ. However, the impact of CAPE on levels of myeloperoxidases (MPO) and pro-inflammatory cytokines during inflammation is not clear...
May 20, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28527800/from-pre-to-postweaning-transformation-of-the-young-calf-s-gastrointestinal-tract
#12
Sarah J Meale, Frederique Chaucheyras-Durand, Harma Berends, Le Luo Guan, Michael A Steele
The ruminant gastrointestinal tract (GIT) faces the challenge of protecting the host from luminal contents and pathogens, while supporting the absorption and metabolism of nutrients for growth and maintenance. The GIT of the calf in early life undergoes some of the most rapid microbial and structural changes documented in nature, and these adaptations in GIT function make the young calf susceptible to GIT diseases and disorders. Despite these challenges, the calf's GIT has a certain degree of plasticity and can sense nutrient supply and respond to bioactive ingredients...
May 17, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/28525373/aquaporins-1-3-and-8-expression-in-irritable-bowel-syndrome-rats-colon-via-nf-%C3%AE%C2%BAb-pathway
#13
Guanqun Chao, Shuo Zhang
OBJECTIVE: Our research was to detect the expression of aquaporins. NF-κB in Irritable bowel syndrome (IBS) rat models' colon so as to find novel pathogenesisof IBS. RESULTS: The expression of AQP1, AQP3, and AQP8 of IBS model group was down-regulated while NF-κB p65 was up-regulated comparing with control group (p < 0.05), and the expression of AQP1, AQP3, and AQP8 of inhibitor group was up-regulated while NF-κB p65 was down-regulated comparing with IBS model group (p < 0...
May 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28523633/synthesis-comparison-and-optimization-of-a-humic-acid-quat10-polyelectrolyte-complex-by-complexation-precipitation-versus-extrusion-spheronization
#14
Margaret Siyawamwaya, Yahya E Choonara, Pradeep Kumar, Pierre P D Kondiah, Lisa C du Toit, Viness Pillay
A novel humic acid and polyquaternium-10 polyelectrolyte complex (PEC) was synthesized utilizing two methods and the solubility and permeability of efavirenz (EFV) were established. Complexation-precipitation and extrusion-spheronization were used to synthesize and compare the drug-loaded PECs. The chemical integrity, thermo-mechanical differences, and morphology between the drug-loaded PECs produced by the two methods were assessed by attenuated total reflectance-Fourier transform infrared, differential scanning calorimetry, and SEM...
May 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28522975/hypoxia-and-inactivity-related-physiological-changes-constipation-inflammation-are-not-reflected-at-the-level-of-gut-metabolites-and-butyrate-producing-microbial-community-the-planhab-study
#15
Robert Šket, Nicole Treichel, Tadej Debevec, Ola Eiken, Igor Mekjavic, Michael Schloter, Marius Vital, Jenna Chandler, James M Tiedje, Boštjan Murovec, Zala Prevoršek, Blaž Stres
We explored the assembly of intestinal microbiota in healthy male participants during the run-in (5 day) and experimental phases [21-day normoxic bed rest (NBR), hypoxic bedrest (HBR)], and hypoxic ambulation (HAmb) in a strictly controlled laboratory environment, balanced fluid, and dietary intakes, controlled circadian rhythm, microbial ambiental burden, and 24/7 medical surveillance. The fraction of inspired O2 (FiO2) and partial pressure of inspired O2 (PiO2) were 0.209 and 133.1 ± 0.3 mmHg for NBR and 0...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28520587/complementary-roles-of-nod2-in-hematopoietic-and-nonhematopoietic-cells-in-preventing-gut-barrier-dysfunction-dependent-on-mlck-activity
#16
Ziad Al Nabhani, Nicolas Montcuquet, Maryline Roy, Monique Dussaillant, Jean-Pierre Hugot, Frédérick Barreau
BACKGROUND: Crohn's disease (CD) pathogenesis is multifactorial involving genetic and environmental factors. Loss of function mutations in the nucleotide oligomerization domain 2 (NOD2) gene are the main genetic risk factor for CD. Like patients with CD, Nod2 mice are characterized by an enhanced Th1 immune response and a defective mucosal barrier function evidenced by increased intestinal permeability. We previously showed that the latter is related to hematopoietic Nod2 deficiency. Our aim was to explore the mechanisms by which Nod2 expressed in the hematopoietic and in the nonhematopoietic compartments interplay to control epithelial paracellular permeability...
May 16, 2017: Inflammatory Bowel Diseases
https://www.readbyqxmd.com/read/28516414/optimized-mucoadhesive-coated-niosomes-as-a-sustained-oral-delivery-system-of-famotidine
#17
Al-Zahraa M Khalifa, Bazigha K Abdul Rasool
The objective of this study is to develop an oral formulation of famotidine niosomes coated with a mucoadhesive polymer, chitosan. Famotidine (FMT) has low oral bioavailability of 40-45% and short half-life between 2.5 to 4 h. Famotidine is classified as class IV in BCS because of its low aqueous solubility (0.1% w/v) and low permeability. Thus, FMT was loaded to the bioadhesive coated niosomes to improve its solubility, enhance its oral bioavailability, and sustain FMT release pattern. Different formulations were prepared by thin-film hydration method and characterized in terms of entrapment efficiency, morphological features, vesicle size, and zeta potential...
May 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28516359/evolution-of-choice-of-solubility-and-dissolution-media-after-two-decades-of-biopharmaceutical-classification-system
#18
Nadia Bou-Chacra, Katherine Jasmine Curo Melo, Ivan Andrés Cordova Morales, Erika S Stippler, Filippos Kesisoglou, Mehran Yazdanian, Raimar Löbenberg
The introduction of the biopharmaceutics drug classification system (Biopharmaceutics Classification System (BCS)), in 1995, provided a simple way to describe the biopharmaceutics behavior of a drug. Solubility and permeability are among the major parameters, which determine the fraction dose absorbed of a drug substance and consequently its chances to be bioavailable. The purpose of this review is to summarize the evolution of the media used for determining solubility and dissolution and how this can be used in modern drug development...
May 17, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28515165/zinc-supplementation-via-gpr39-upregulates-pkc%C3%AE-to-protect-intestinal-barrier-integrity-in-caco-2-cells-challenged-by-salmonella-enterica-serovar-typhimurium
#19
Yu-Xin Shao, Zhao Lei, Patricia G Wolf, Yan Gao, Yu-Ming Guo, Bing-Kun Zhang
Background: Zinc has been shown to improve intestinal barrier function against Salmonella enterica serovar Typhimurium (S. typhimurium) infection, but the mechanisms involved in this process remain undefined.Objective: We aimed to explore the roles of G protein-coupled receptor (GPR)39 and protein kinase Cζ (PKCζ) in the regulation by zinc of intestinal barrier function.Methods: A Transwell Caco-2 monolayer was pretreated with 0, 50, or 100 μM Zn and then incubated with S. typhimurium for 0-6 h. Afterward, cells silenced by the small interfering RNA for GPR39 or PKCζ were pretreated with 100 μM Zn and incubated with S...
May 17, 2017: Journal of Nutrition
https://www.readbyqxmd.com/read/28514703/bacterial-infections-and-hepatic-encephalopathy-in-liver-cirrhosis-prophylaxis-and-treatment
#20
REVIEW
Damian Piotrowski, Anna Boroń-Kaczmarska
Infections are common among patients with liver cirrhosis. They occur more often in cirrhotic patient groups than in the general population and result in higher mortality. One reason for this phenomenon is bacterial translocation from the intestinal lumen that occurs as a consequence of intestinal bacterial overgrowth, increased permeability and decreased motility. The most common infections in cirrhotic patients are spontaneous bacterial peritonitis and urinary tract infections, followed by pneumonia, skin and soft tissue infections...
May 14, 2017: Advances in Medical Sciences
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