Intestinal Absorption Mechanism of Mirabegron, a Potent and Selective β3-Adrenoceptor Agonist: Involvement of Human Efflux and/or Influx Transport Systems

2013 ◽  
Vol 10 (5) ◽  
pp. 1783-1794 ◽  
Author(s):  
Shin Takusagawa ◽  
Fumihiko Ushigome ◽  
Hiroyuki Nemoto ◽  
Yutaka Takahashi ◽  
Qun Li ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Transport Systems ◽  
Absorption Mechanism ◽  
Adrenoceptor Agonist ◽  
Influx Transport

scholarly journals New In Vitro Coculture Model for Evaluating Intestinal Absorption of Different Lipid Nanocapsules

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 595
Author(s):  
Norraseth Kaeokhamloed ◽  
Emillie Roger ◽  
Jérôme Béjaud ◽  
Nolwenn Lautram ◽  
Florence Manero ◽  
...  
Keyword(s):  
Surface Modification ◽  
Intestinal Absorption ◽  
Oral Absorption ◽  
Membrane Integrity ◽  
Microvascular Endothelial Cell ◽  
Absorption Mechanism ◽  
Apparent Permeability ◽  
Lipid Nanocapsules ◽  
Coculture Model

Standard models used for evaluating the absorption of nanoparticles like Caco-2 ignore the presence of vascular endothelium, which is a part of the intestinal multi-layered barrier structure. Therefore, a coculture between the Caco-2 epithelium and HMEC-1 (Human Microvascular Endothelial Cell type 1) on a Transwell® insert has been developed. The model has been validated for (a) membrane morphology by transmission electron microscope (TEM); (b) ZO-1 and β-catenin expression by immunoassay; (c) membrane integrity by trans-epithelial electrical resistance (TEER) measurement; and (d) apparent permeability of drugs from different biopharmaceutical classification system (BCS) classes. Lipid nanocapsules (LNCs) were formulated with different sizes (55 and 85 nm) and surface modifications (DSPE-mPEG (2000) and stearylamine). Nanocapsule integrity and particle concentration were monitored using the Förster resonance energy transfer (FRET) technique. The result showed that surface modification by DSPE-mPEG (2000) increased the absorption of 55-nm LNCs in the coculture model but not in the Caco-2. Summarily, the coculture model was validated as a tool for evaluating the intestinal absorption of drugs and nanoparticles. The new coculture model has a different LNCs absorption mechanism suggesting the importance of intestinal endothelium and reveals that the surface modification of LNCs can modify the in vitro oral absorption.

Baclofen: Intestinal absorption mechanism in mice

1996 ◽  
Vol 27 (7) ◽  
pp. 1269-1271 ◽  
Author(s):  
Graciela N. Balerio ◽  
Modesto C. Rubio
Keyword(s):  
Intestinal Absorption ◽  
Absorption Mechanism

Lipid Absorption and Deposition in Rainbow Trout (Salmo gairdnerii)

1973 ◽  
Vol 51 (7) ◽  
pp. 1050-1058 ◽  
Author(s):  
J. Stephen Robinson ◽  
James F. Mead
Keyword(s):  
Fatty Acids ◽  
Rainbow Trout ◽  
Palmitic Acid ◽  
Free Fatty Acids ◽  
Intestinal Absorption ◽  
Lipid Absorption ◽  
Portal System ◽  
Absorption Mechanism ◽  
Dark Muscle ◽  
Muscle Lipids

Rainbow trout, fed or starved for 5 weeks, were force-fed 23 μCi 1-14C-palmitic acid and sacrificed at [Formula: see text], 1, 2, 4, 8, and 14 h after feeding. Analysis of the blood suggested that trout possess an intestinal absorption mechanism for lipid that is very different from that found in other animals. The fish, incapable of delivering triglyceride to its circulation in the usual way, receives most of its absorbed lipid as free fatty acids, probably via the portal system. It was also found that light muscle more easily yielded its triglyceride stores, in agreement with its role as the major lipid depot in trout. Nonetheless, dark muscle was metabolically more active in deposition of muscle lipids. Dark muscle appeared to function more as an organ than a kinetically responsible contractile body.

scholarly journals Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles

2019 ◽  
Vol Volume 14 ◽  
pp. 9721-9730 ◽  
Author(s):  
Yike Huang ◽  
Suya Deng ◽  
Xinxin Luo ◽  
Yi Liu ◽  
Wanjun Xu ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Absorption Mechanism ◽  
Albumin Nanoparticles

scholarly journals Erratum for: Elucidation of the Intestinal Absorption Mechanism of Celastrol Using the Caco-2 Cell Transwell Model

Planta Medica ◽  
2016 ◽  
Vol 82 (13) ◽  
pp. E6-E6
Author(s):  
Hong Li ◽  
Jie Li ◽  
Lu Liu ◽  
Yichuan Zhang ◽  
Yili Luo ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Absorption Mechanism

scholarly journals Species Difference in Intestinal Absorption Mechanism of Etoposide and Digoxin between Cynomolgus Monkey and Rat

2008 ◽  
Vol 25 (11) ◽  
pp. 2467-2476 ◽  
Author(s):  
T. Nishimura ◽  
Y. Kato ◽  
N. Amano ◽  
M. Ono ◽  
Y. Kubo ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Cynomolgus Monkey ◽  
Species Difference ◽  
Absorption Mechanism

scholarly journals In vitro and in situ study on characterizationand mechanismofthe intestinal absorptionof 2,3,5,4'-tetrahydroxy-stilbene-2-O-β-D-glucoside

2020 ◽  
Author(s):  
Cheng Wang ◽  
Yimeng Zhou ◽  
Xiaohong Gong ◽  
Li Zheng ◽  
Yunxia Li
Keyword(s):  
Intestinal Absorption ◽  
High Performance ◽  
Cell Monolayer ◽  
Absorption Mechanism ◽  
Pharmacological Activities ◽  
Concentration Time ◽  
In Situ Experiments ◽  
Basic Parameters

Abstract Background: 2,3,5,4'-tetrahydroxystilbence-2-O-β-D-glucoside(TSG) is a polyhydroxyphenolic compound, which exhibited a broad spectrum of pharmacological activities, such asanti-inflammatory, anti-depression, anti-oxidation and anti-atherosclerosis.However, the compound had poor bioavailability and the underlying absorption mechanisms had not been studied. Therefore, the purpose of this study was to investigate the intestinal absorption mechanism of TSG. Methods: This study used Caco-2 cell monolayer model and single-passintestinal perfusion modelto explore the gastrointestinal absorption mechanisms of TSG. The effects of basic parameters such as drug concentration, time and pH on the intestinal absorption of TSG were analyzed by high performance liquid chromatography.The absorption susceptibility of TSG to three inhibitors, P-gp inhibitors verapamil hydrochloride and quinidine, and MRP2 inhibitor probenecid were also assessed. Results: TSG was poorly absorbed in the intestines and the absorption of TSG in stomach is much higher than that in intestine. Both in vitro and in situ experiments showed that the absorption of TSG was saturated with increasing concentration and it was better absorbed in a weakly acidic environment pH 6.4. Moreover, TSG interacts with P-gp and MRP2, and TSG was not only the substrate of the P-gp and MRP2, but also affected the expression of P-gp and MRP2. Conclusions: It wasconcluded that the gastrointestinalabsorption mechanisms ofTSG involved processes passive transport and the participation ofefflux transporters.

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