scholarly journals Enhanced Transepithelial Permeation of Gallic Acid and (−)-Epigallocatechin Gallate across Human Intestinal Caco-2 Cells Using Electrospun Xanthan Nanofibers

Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 155 ◽  
Author(s):  
Adele Faralli ◽  
Elhamalsadat Shekarforoush ◽  
Ana Mendes ◽  
Ioannis Chronakis
Keyword(s):  
Gallic Acid ◽  
Epigallocatechin Gallate ◽  
Electrospun Nanofibers ◽  
Transepithelial Transport ◽  
Efflux Transporters ◽  
Polyphenol Compounds ◽  
Cell Monolayers ◽  
Permeability Enhancement ◽  
Release Studies

Electrospun xanthan polysaccharide nanofibers (X) were developed as an encapsulation and delivery system of the poorly absorbed polyphenol compounds, gallic acid (GA) and (−)-epigallocatechin gallate (EGCG). Scanning electron microscopy was used to characterize the electrospun nanofibers, and controlled release studies were performed at pH 6.5 and 7.4 in saline buffer, suggesting that the release of polyphenols from xanthan nanofibers follows a non Fickian mechanism. Furthermore, the X-GA and X-EGCG nanofibers were incubated with Caco-2 cells, and the cell viability, transepithelial transport, and permeability properties across cell monolayers were investigated. An increase of GA and EGCG permeability was observed when the polyphenols were loaded into xanthan nanofibers, compared to the free compounds. The observed in vitro permeability enhancement of GA and EGCG was induced by the presence of the polysaccharide nanofibers, which successfully inhibited efflux transporters, as well as by tight junctions opening.

scholarly journals Interaction between Miltefosine and Amphotericin B: Consequences for Their Activities towards Intestinal Epithelial Cells and Leishmania donovani Promastigotes In Vitro

2006 ◽  
Vol 50 (11) ◽  
pp. 3793-3800 ◽  
Author(s):  
Cécile Ménez ◽  
Marion Buyse ◽  
Madeleine Besnard ◽  
Robert Farinotti ◽  
Philippe M. Loiseau ◽  
...  
Keyword(s):  
Amphotericin B ◽  
Leishmania Donovani ◽  
Biological Activities ◽  
Intestinal Barrier ◽  
Oral Route ◽  
Transepithelial Transport ◽  
Physicochemical Interaction ◽  
Cell Monolayers ◽  
Permeability Enhancement

ABSTRACT The aim of this study was to evaluate the potential of a combination of two antileishmanial drugs, miltefosine (HePC) and amphotericin B (AMB), when administered by the oral route. Caco-2 cell monolayers were used as a validated in vitro model of the intestinal barrier and Leishmania donovani promastigotes as a model for evaluating the effect of the drug combination. Spectroscopic measurements demonstrated that HePC and AMB associate, leading to the formation of mixed aggregates in which AMB is solubilized as monomers. The incubation of the association of HePC and AMB with Caco-2 cell monolayers, at a concentration higher than 5 μM, led to (i) a reduction of the HePC-induced paracellular permeability enhancement in Caco-2 cell monolayers, (ii) an inhibition of the uptake of both drugs, and (iii) a decrease in the transepithelial transport of both drugs, suggesting that a pharmacokinetic antagonism between HePC and AMB could occur after their oral administration. However, the combination did not exhibit any antagonism or synergy in its antileishmanial activity. These results demonstrated a strong physicochemical interaction between HePC and AMB, depending on the concentration of each, which could have important consequences for their biological activities, if they are administered together.

scholarly journals Relevance and Standardization of In Vitro Antioxidant Assays: ABTS, DPPH, and Folin–Ciocalteu

2018 ◽  
Vol 2018 ◽  
pp. 1-9 ◽  
Author(s):  
Helena Abramovič ◽  
Blaž Grobin ◽  
Nataša Poklar Ulrih ◽  
Blaž Cigić
Keyword(s):  
Ascorbic Acid ◽  
Chlorogenic Acid ◽  
Gallic Acid ◽  
Caffeic Acid ◽  
Sulfonic Acid ◽  
Epigallocatechin Gallate ◽  
The Other ◽  
Oh Groups ◽  
Standard Compound

Trolox, gallic acid, chlorogenic acid, caffeic acid, catechin, epigallocatechin gallate, and ascorbic acid are antioxidants used as standards for reaction with chromogenic radicals, 2,2-diphenyl-1-picrylhydrazyl (DPPH⋅) and 2,2′-azino-bis-3-ethylbenzotiazolin-6-sulfonic acid (ABTS⋅+), and Folin–Ciocalteu (FC) reagent. The number of exchanged electrons has been analyzed as function of method and solvent. A majority of compounds exchange more electrons in FC assay than in ABTS and DPPH assays. In reaction with chromogenic radicals, the largest number of electrons was exchanged in buffer (pH 7.4) and the lowest reactivity was in methanol (DPPH) and water (ABTS). At physiological pH, the number of exchanged electrons of polyphenols exceeded the number of OH groups, pointing to the important contribution of partially oxidized antioxidants, formed in the course of reaction, to the antioxidant potential. For Trolox, small impact on the number of exchanged electrons was observed, confirming that it is more suitable as a standard compound than the other antioxidants.

Transepithelial phosphate transport in rabbit proximal tubular cells adapted to phosphate deprivation

1994 ◽  
Vol 266 (6) ◽  
pp. C1609-C1618 ◽  
Author(s):  
S. J. Scheinman ◽  
R. Reid ◽  
R. Coulson ◽  
D. B. Jones ◽  
S. M. Ford
Keyword(s):  
Primary Cultures ◽  
Phosphate Transport ◽  
Progressive Increase ◽  
Transepithelial Transport ◽  
Cortical Cells ◽  
Cell Monolayers ◽  
Pi Transport ◽  
Overnight Incubation ◽  
Proximal Tubular

Both renal and nonrenal cells in culture adapt to deprivation of Pi by increasing Na-dependent Pi uptake. We studied whether this change in uptake is reflected in an increased renal transepithelial Pi transport. We grew primary cultures of rabbit renal cortical cells in plastic flasks and subcultured them onto Millicell-HA filters. This produced cell monolayers, which structurally and functionally resembled proximal tubule. These cells performed Na-dependent net transepithelial transport of 32Pi in the apical-to-basolateral direction that was inhibited by phosphonoformic acid in the apical fluid or by ouabain in the basolateral fluid or by preincubation with parathyroid hormone. Overnight incubation at low Pi concentrations led to a progressive increase in 5-min Na-dependent Pi uptake into cell monolayers. Na-dependent Pi uptake was threefold higher following overnight incubation at 25 microM Pi, compared with 3 mM Pi, and the increase was one-half maximal with incubation at an extracellular Pi concentration ([Pi]) of 300 microM. This was associated with a decrease in Na-dependent transepithelial Pi flux to the basolateral fluid by the same cells, which fell dramatically following incubation at < or = 300 microM Pi. There was no change in Na-dependent uptake or transepithelial transport of L-glutamine. This adaptation to Pi deprivation in vitro appears to serve to restore depleted cell stores of Pi rather than to regulate transepithelial Pi transport.

scholarly journals Bioactive Multilayer Polylactide Films with Controlled Release Capacity of Gallic Acid Accomplished by Incorporating Electrospun Nanostructured Coatings and Interlayers

2019 ◽  
Vol 9 (3) ◽  
pp. 533 ◽  
Author(s):  
Luis Quiles-Carrillo ◽  
Nestor Montanes ◽  
José Lagaron ◽  
Rafael Balart ◽  
Sergio Torres-Giner
Keyword(s):  
Sustained Release ◽  
Gallic Acid ◽  
In Vitro Release ◽  
The Other ◽  
High Transparency ◽  
Release Capacity ◽  
Release Studies ◽  
Vitro Release ◽  
Saline Medium

The present research reports on the development of bi- and multilayer polylactide (PLA) films by the incorporation of electrospun nanostructured PLA coatings and interlayers containing the antioxidant gallic acid (GA) at 40 wt% onto cast-extruded PLA films. To achieve the bilayer structures, submicron GA-loaded PLA fibers were applied on 200-µm cast PLA films in the form of coatings by electrospinning for 1, 2, and 3 h. For the multilayers, the cast PLA films were first coated on one side by electrospinning, then sandwiched with 10-µm PLA film on the other side, and the resultant whole structure was finally thermally post-treated at 150 °C without pressure. Whereas the bilayer PLA films easily delaminated and lacked transparency, the multilayers showed sufficient adhesion between layers and high transparency for deposition times during electrospinning of up to 2 h. The incorporation of GA positively contributed to delaying the thermal degradation of PLA for approximately 10 °C, as all films were thermally stable up to 345 °C. The in vitro release studies performed in saline medium indicated that the GA released from the bilayer PLA films rapidly increased during the first 5 h of immersion while it stabilized after 45–250 h. Interestingly, the PLA multilayers offered a high sustained release of GA, having the capacity to deliver the bioactive for over 1000 h. In addition, in the whole tested period, the GA released from the PLA films retained most of its antioxidant functionality. Thus, during the first days, the bilayer PLA films can perform as potent vehicles to deliver GA while the multilayer PLA films are able to show a sustained release of the natural antioxidant for extended periods.

Transepithelial Transport ofp-Coumaric Acid and Gallic Acid in Caco-2 Cell Monolayers

2003 ◽  
Vol 67 (11) ◽  
pp. 2317-2324 ◽  
Author(s):  
Yutaka KONISHI ◽  
Shoko KOBAYASHI ◽  
Makoto SHIMIZU
Keyword(s):  
Gallic Acid ◽  
Transepithelial Transport ◽  
Coumaric Acid ◽  
Cell Monolayers

Transepithelial transport mechanisms of 7,8-dihydroxyflavone, a small molecular TrkB receptor agonist, in human intestinal Caco-2 cells

2019 ◽  
Vol 10 (8) ◽  
pp. 5215-5227 ◽  
Author(s):  
Yufeng Chen ◽  
Fan Xue ◽  
Guobin Xia ◽  
Zhenlei Zhao ◽  
Chun Chen ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Transepithelial Transport ◽  
Efflux Transporters ◽  
Transport Mechanisms ◽  
Passive Transport ◽  
Cell Monolayers ◽  
Trkb Receptor

7,8-DHF was transported across Caco-2 cell monolayers by passive transport with carrier-mediated influx and efflux transporters.

scholarly journals Effect of luminal flow on doming of mpkCCD cells in a 3D perfusable kidney cortical collecting duct model

2020 ◽  
Vol 319 (1) ◽  
pp. C136-C147
Author(s):  
Joshua L. Rein ◽  
Szilvia Heja ◽  
Daniel Flores ◽  
Rolando Carrisoza-Gaytán ◽  
Neil Y. C. Lin ◽  
...  
Keyword(s):  
Collecting Duct ◽  
Three Dimensional ◽  
Transepithelial Transport ◽  
Cortical Collecting Duct ◽  
Acid Base ◽  
Cell Monolayers ◽  
Luminal Flow ◽  
Total Body ◽  
Epithelial Sheets

The cortical collecting duct (CCD) of the mammalian kidney plays a major role in the maintenance of total body electrolyte, acid/base, and fluid homeostasis by tubular reabsorption and excretion. The mammalian CCD is heterogeneous, composed of Na+-absorbing principal cells (PCs) and acid-base-transporting intercalated cells (ICs). Perturbations in luminal flow rate alter hydrodynamic forces to which these cells in the cylindrical tubules are exposed. However, most studies of tubular ion transport have been performed in cell monolayers grown on or epithelial sheets affixed to a flat support, since analysis of transepithelial transport in native tubules by in vitro microperfusion requires considerable expertise. Here, we report on the generation and characterization of an in vitro, perfusable three-dimensional kidney CCD model (3D CCD), in which immortalized mouse PC-like mpkCCD cells are seeded within a cylindrical channel embedded within an engineered extracellular matrix and subjected to luminal fluid flow. We find that a tight epithelial barrier composed of differentiated and polarized PCs forms within 1 wk. Immunofluorescence microscopy reveals the apical epithelial Na+ channel ENaC and basolateral Na+/K+-ATPase. On cessation of luminal flow, benzamil-inhibitable cell doming is observed within these 3D CCDs consistent with the presence of ENaC-mediated Na+ absorption. Our 3D CCD provides a geometrically and microphysiologically relevant platform for studying the development and physiology of renal tubule segments.

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