Evaluation of the appropriate time range for estimating the apparent permeability coefficient (Papp) in a transcellular transport study

Ozeki, Kazuhisa; Kato, Motohiro; Sakurai, Yuuji; Ishigai, Masaki; Kudo, Toshiyuki; Ito, Kiyomi

doi:10.1016/j.ijpharm.2015.09.035

Cited by 11 publications

(7 citation statements)

References 22 publications

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“…In transcellular studies, apparent permeability coefficient (Papp) was used to represent the amount of compound transported per unit time (Wang et al, 2017a). It was reported that the value of Papp is correlated to the extent of drug molecules that penetrate across the intestinal tract of the drugs (Artursson and Karlsson, 1991;Ozeki et al, 2015;). However, in another curcumin permeability study conducted using Caco-2 cell line it was reported that efflux pathways do not play a role in curcumin intestinal permeability.…”

Section: Low Permeability (Absorption)mentioning

confidence: 99%

Recent developments in formulation design for improving oral bioavailability of curcumin: A review

Liu

Smart

Pannala

2020

Journal of Drug Delivery Science and Technology

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Curcumin, a yellow-orange substance that is extracted from the spice turmeric (Curcuma longa, Zinziberaceae), has been attributed with a wide range of pharmacological activities for the prevention and treatment of several disease conditions such as arthritis, hypertension, diabetes, Alzheimer's, antibacterial and cancer to name a few. However, its potential for use as an orally delivered medicinal product is hindered by its poor solubility and bioavailability. The low oral bioavailability of curcumin is caused by several factors including low aqueous solubility, poor intestinal permeability, unstable at alkaline pH and rapid metabolism. To improve curcumin's poor oral bioavailability, different formulation strategies such as incorporation into nanoparticles, liposomes, micelles, micro/nano-emulsions and solid dispersions as well as coadministration with piperine have been investigated in both animal models as well as human supplementation studies. In this review, novel formulations of curcumin for oral delivery that were developed in recent years are reviewed and discussed.

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Section: Low Permeability (Absorption)mentioning

confidence: 99%

Recent developments in formulation design for improving oral bioavailability of curcumin: A review

Liu

Smart

Pannala

2020

Journal of Drug Delivery Science and Technology

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“…The kit is based on the measurement of oxidized o-dianisidine (pink) produced through the following chemical reactions , , and . The consequent increase of oxidized o-dianisidine (pink) in absorbance at 540 nm measured by a SpectraMax i3 Platform spectrophotometer (Molecular Devices, Austria) was directly proportional to the glucose concentration. The apparent permeability coefficient ( P app , cm/s) of glucose transport from apical to the basal compartment was calculated according to the following equation where d Q /d t is a steady-state flux (μg/s), A is the surface area of the inset (cm 2 ), and C 0 is the initial concentration in the apical compartment (μg/cm 3 ) …”

Section: Materials and Methodsmentioning

confidence: 99%

“…where dQ/dt is a steady-state flux (μg/s), A is the surface area of the inset (cm 2 ), and C 0 is the initial concentration in the apical compartment (μg/cm 3 ). 30 2.5. Assay of Glucose Uptake in Caco-2 Cells.…”

Section: Methodsmentioning

confidence: 99%

Extract of Unifloral Camellia sinensis L. Pollen Collected by Apis mellifera L. Honeybees Exerted Inhibitory Effects on Glucose Uptake and Transport by Interacting with Glucose Transporters in Human Intestinal Cells

Ren

Yan

et al. 2021

J. Agric. Food Chem.

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Bee pollen possesses potential hypoglycemic effects but its inhibitory mechanisms on glucose absorption and transportation in intestinal cells still need to be clarified. Here, we determined the inhibitory effects of bee pollen extract originating from Camellia sinensis L. (BP-Cs) as well as its representative phenolic compounds on glucose uptake and transport through a human intestinal Caco-2 cell monolayer model. It showed that three representative phenolic compounds, including gallic acid (GA), ), with contents of 27.7 ± 0.86, 9.88 ± 0.54, and 7.83 ± 0.46 μg/mg in BP-Cs extract, respectively, exerted mutual antagonistic actions interacting with glucose transporters to inhibit glucose uptake and transport based on their combination index (CI) and molecular docking analysis. K1, K2, and GA might compete with D-glucose to form hydrogen bonds with the same active residues including GLU-412, GLY-416, GLN-314, and TRP-420 in GLUT2. These findings provide us a deep understanding of the mechanisms underlying the anti-hyperglycemia by bee pollen, which provide a new sight on dietary intervention strategies against diabetes.

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“…Evaluation of the apparent permeability coefficient (P app ) in a transcellular transport study is widely used in drug development to predict drug absorption in humans. 1,2) The lag often shown before reaching the linear range in the receiver compartment limits the range of the linear phase, [3][4][5] and several proposals have been made to modify the equation to overcome the issue in calculating P app . 2,4) However, these approaches are not often applied because the calculations are complex.…”

Section: Introductionmentioning

confidence: 99%

“…1,2) The lag often shown before reaching the linear range in the receiver compartment limits the range of the linear phase, [3][4][5] and several proposals have been made to modify the equation to overcome the issue in calculating P app . 2,4) However, these approaches are not often applied because the calculations are complex. 2) There are several reports of using three-compartment model analysis in a transcellular transport assay to analyze the concentration profiles.…”

Section: Introductionmentioning

confidence: 99%

Three-Compartment Model Analysis with Minimal Sampling Points in the Caco-2 Permeability Assay

Nagayasu

Ozeki

Onoue

2019

Biological & Pharmaceutical Bulletin

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The purpose of this study was to establish a modified method of three-compartment model analysis that minimized the sampling frequency. A Caco-2 permeability assay was performed on ten structurally diverse compounds with passive diffusion. A three-compartment model was analyzed by a conventional method and a method with fewer sampling points, called the simplified method, using concentration-time profiles in the donor, intracellular, and receiver compartments. The concentration-time profiles in all compartments were well described by the conventional method. The calculated unbound fraction of intracellular (fu 2) and apparent permeability coefficient (P app) were 0.0107-1.22 and 0.886-146 10 6 cm/s, respectively. The simplified method also described the concentration profiles in the compartments of all ten compounds except one, ibuprofen. The difference in values calculated by the simplified method compared to the conventional method was between 7 and 7% for fu 2 and between 6 and 42% for P app. These results suggested that the parameter values from the simplified method were comparable with those from the conventional method. The simplified method may be a promising approach to improve the throughput of three-compartment model analyses of Caco-2 permeability assays in the early stages of drug discovery.

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Evaluation of the appropriate time range for estimating the apparent permeability coefficient (Papp) in a transcellular transport study

Cited by 11 publications

References 22 publications

Recent developments in formulation design for improving oral bioavailability of curcumin: A review

Recent developments in formulation design for improving oral bioavailability of curcumin: A review

Extract of Unifloral Camellia sinensis L. Pollen Collected by Apis mellifera L. Honeybees Exerted Inhibitory Effects on Glucose Uptake and Transport by Interacting with Glucose Transporters in Human Intestinal Cells

Three-Compartment Model Analysis with Minimal Sampling Points in the Caco-2 Permeability Assay

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