An Overview of Caco‐2 and Alternatives for Prediction of Intestinal Drug Transport and Absorption

Ungell, Anna‐Lena; Artursson, Per

doi:10.1002/9783527623860.ch7

Cited by 12 publications

(15 citation statements)

References 139 publications

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“…In agreement with the theory behind the Caco‐2 cell model assay (Ungell & Artursson, ), the high value of apparent permeability coefficient found for the isotonic mixture ( P app > 10 −5 cm s −1 ) suggests that amino acids extracted from codfish salting wastewater are likely to be absorbed in vivo by the human intestine and do not alter intestinal cell's integrity. Salt was demonstrated to have an important role, increasing transport and permeability of amino acids with respect to the unsalted solution.…”

Section: Discussionsupporting

confidence: 81%

“…Due to the importance of dietary amino acids, it is crucial to evaluate their bioavailability, that is, the capability to be taken up by a specific tissue or organ after administration. Dietary amino acids become available to the cells of specific tissues and organs once in the blood circulation after permeating the intestinal wall (Ungell & Artursson, ). Dietary amino acids also have important functions in the intestine; they are major fuel for the small intestinal mucosa (epithelium) and are obligatory precursors for intestinal syntheses of glutathione, nitric oxide, polyamines, purine and pyrimidine nucleotides and some other important compounds (Wu, ).…”

Section: Introductionmentioning

confidence: 99%

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In vitro intestinal absorption of amino acid mixtures extracted from codfish (Gadus morhua L.) salting wastewater

Ferraro

Jorge

Cruz

et al. 2013

Int J of Food Sci Tech

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This study reports on the intestinal permeability of salt-containing mixtures of amino acids extracted from codfish salting wastewater. Permeability was evaluated in vitro using the Caco-2 cell line model; cell integrity during exposure to mixtures of amino acids was estimated by measuring the transepithelial electrical resistance (TEER). The effect of salt (NaCl) on the permeability and on the intestinal cell's integrity was also examined. Permeation rate (i.e. transport) was ≥95% for all amino acids except for creatine, for which it was 6%. Values for apparent permeability coefficients, P app > 10 À5 cm s À1 , for mixture with isotonic concentration of NaCl suggest that amino acids are very likely to be absorbed in humans. Mixture with a hypertonic level of NaCl exerts a cytotoxic effect in intestinal cells resulting in a loss of epithelium integrity. Results show that isotonic mixture of amino acids extracted from codfish salting wastewater could be used in food, feed, cosmetic and pharmaceutical formulations. These applications could contribute to the fish industry sustainability. Amino acid intestinal absorption V. Ferraro et al. Amino acid intestinal absorption V. Ferraro et al. Amino acid intestinal absorption V. Ferraro et al. Amino acid intestinal absorption V. Ferraro et al. Amino acid intestinal absorption V. Ferraro et al.

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Section: Discussionsupporting

confidence: 81%

Section: Introductionmentioning

confidence: 99%

In vitro intestinal absorption of amino acid mixtures extracted from codfish (Gadus morhua L.) salting wastewater

Ferraro

Jorge

Cruz

et al. 2013

Int J of Food Sci Tech

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“…The primary in vitro tool for assessing absorption is the cell-based Caco-2 permeability assay (Artursson and Karlsson, 1991;Artursson et al, 2001;Ungell and Artursson, 2009), although Madin-Darby canine kidney cells transfected with the multidrug resistance 1 polypeptide (MDR1) gene (MDCK-MDR1), parallel artificial membrane permeability assay (PAMPA), or in silico predictions may also provide valuable information about efflux-transporter risk and permeability (Tang et al, 2002;Avdeef, 2005). This permeability assessment, in combination with a solubility measurement (ideally Drug Metabolism Reviews Downloaded from informahealthcare.com by University of S.A Lib 119257 on 10/19/12…”

Section: Tactical Approaches To Absorption and Bioavailabilitymentioning

confidence: 99%

The right compound in the right assay at the right time: an integrated discovery DMPK strategy

Ballard

Brassil

Bui

et al. 2012

Drug Metabolism Reviews

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“…Different cell types were used to answer different questions on, e.g., passive transport, active transport, transporter specificity, etc. The Caco-2 cell layer permeability is the most popular method in this respect [17]. The artificial-membrane technology is used to measure passive permeation through membranes composed of mixtures of phospholipids in dodecane, supported by an inert polycarbonate filter membrane [18] [19].…”

Section: The Intestinalmentioning

confidence: 99%

Measurement and Prediction of Oral Absorption

Keldenich

2009

Chemistry & Biodiversity

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After defining oral absorption, this review article summarizes the influence of different physiological and physicochemical parameters on oral absorption explained according to the situation at BayerScheringPharma. Along the optimization process in industries, prediction of oral absorption is exemplified. In silico prediction of oral absorption in early stages of research is highlighted with three examples, i.e., a classification algorithm, a single parameter prediction, and a linear free-energy relationship. In vitro prediction of permeation using Caco-2 cell layers and physicochemical modeling is exemplified. The influence of solubility is shown by a concrete example, in particular, using physiologically based pharmacokinetic (PBPK) modeling and physicochemical parameters. For later stages, optimization examples of in vivo animal models stress the importance of excellent in vivo data and in vivo/in vivo correlations for the prediction of human oral absorption from animal experiments.

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An Overview of Caco‐2 and Alternatives for Prediction of Intestinal Drug Transport and Absorption

Cited by 12 publications

References 139 publications

In vitro intestinal absorption of amino acid mixtures extracted from codfish (Gadus morhua L.) salting wastewater

In vitro intestinal absorption of amino acid mixtures extracted from codfish (Gadus morhua L.) salting wastewater

The right compound in the right assay at the right time: an integrated discovery DMPK strategy

Measurement and Prediction of Oral Absorption

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