An HPLC-UV method for the measurement of permeability of marker drugs in the Caco-2 cell assay

Kratz, Jadel M.; Teixeira, Marina Rodrigues; Koester, Letícia Scherer; Simões, Claudia Maria de Oliveira

doi:10.1590/s0100-879x2011007500060

Cited by 22 publications

(14 citation statements)

References 29 publications

(29 reference statements)

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“…The P app values across the Caco-2 cell monolayer for A to B of GG, atenolol, furosemide, carbamazepine, and verapamil were determined. In this study, the P app for QC compounds as well as the permeability rank were comparable with the literature values [10,[15][16][17]. The permeability rank of the test and QC compounds were done according to "low", if P app < 2.5 × 10 − 6 cm/sec, and "high", if P app ≥ 2.50 × 10 − 6 cm/sec.…”

mentioning

confidence: 55%

In Vitro Metabolic Stability and Permeability of Gymnemagenin and Its In Vivo Pharmacokinetic Correlation in Rats – A Pilot Study

et al. 2016

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Gymnema sylvestre is traditionally used for diabetes mellitus. A literature survey revealed very few reports, particularly on rat liver microsomal stability, caco-2 permeability and efflux concerns and its correlation with the bioavailability of gymnemagenin, an important component of G. sylvestre. Therefore, the objective of our study was to investigate the in vitro rat liver microsomal stability and caco-2 permeability along with the efflux of gymnemagenin and establish a probable correlation of these in vitro findings with pharmacokinetic parameters after oral and intravenous administration in rats. Rat liver microsomal stability studies to estimate the in vitro intrinsic half-life, clearance, and Caco-2 permeability after 21 days of culture to determine the apparent permeability from apical to basal and from basal to apical, and efflux ratio of gymnemagenin were performed using liquid chromatography-tandem mass spectrometry. A sensitive, robust bioanalytical method was validated and successfully applied to determine the plasma exposure of gymnemagenin. In vitro rat liver microsomal stability demonstrated that gymnemagenin metabolizes rapidly with a short apparent and intrinsic half-life (~?7?min) and high intrinsic clearance, i.e., 190.08??L/min/mg of microsomes. The results of the Caco-2 study indicated a poor permeability (1.31???10??6?cm/sec) with a very high efflux ratio. The pharmacokinetic study revealed poor oral bioavailability (~?14?%) of gymnemagenin and it was found to have a short half-life and a high clearance in rats. Our in vitro findings indicated low metabolic stability and poor Caco-2 permeability with high efflux, which might have a role in the observed poor oral bioavailability in rats.

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confidence: 55%

In Vitro Metabolic Stability and Permeability of Gymnemagenin and Its In Vivo Pharmacokinetic Correlation in Rats – A Pilot Study

et al. 2016

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“…Thereafter, samples (100 μL) were taken out from the receiver side at 0.5, 1.0, 1.5, 2.0 and 3.0 h, and the equivalent volume of fresh transport medium was supplemented. Finally, all the samples were analyzed by HPLC system [26,27], and free riboflavin laurate was measured by the method developed in our lab.…”

Section: Methodsmentioning

confidence: 99%

Exploration of the Protection of Riboflavin Laurate on Oral Mucositis Induced by Chemotherapy or Radiotherapy at the Cellular Level: What Is the Leading Contributor?

Xuan

Yang

et al. 2013

IJMS

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Oral or gastrointestinal mucositis is a frequent phenomenon in cancer patients receiving chemotherapy or radiotherapy. In addition, several clinical investigations have demonstrated in recent years that riboflavin laurate has the potential to protect the patients from the disease induced by chemotherapy or radiotherapy. In our studies, it is observed that riboflavin laurate can ameliorate either chemotherapy- or radiotherapy-induced toxicities on Helf cells, and the effect is greater than that of riboflavin. In addition, riboflavin laurate is able to transport through the Caco-2 cell monolayer as the prototype, indicating the protective effects may be produced by the prototype of riboflavin laurate, rather than simply by the released riboflavin.

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“…Propranolol is a non-substrate of P-gp and was used as a marker for passive, transcellular transport [22]. Propranolol alone data were not acquired for this particular study as propranolol is commonly used as marker for the transcellular transport known not to be influenced by P-gp and R123.…”

Section: Caco-2 Transport Studiesmentioning

confidence: 99%

P-glycoprotein interactions of novel psychoactive substances – Stimulation of ATP consumption and transport across Caco-2 monolayers

Meyer

Wagmann

Schneider-Daum

et al. 2015

Biochemical Pharmacology

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An HPLC-UV method for the measurement of permeability of marker drugs in the Caco-2 cell assay

Cited by 22 publications

References 29 publications

In Vitro Metabolic Stability and Permeability of Gymnemagenin and Its In Vivo Pharmacokinetic Correlation in Rats – A Pilot Study

In Vitro Metabolic Stability and Permeability of Gymnemagenin and Its In Vivo Pharmacokinetic Correlation in Rats – A Pilot Study

Exploration of the Protection of Riboflavin Laurate on Oral Mucositis Induced by Chemotherapy or Radiotherapy at the Cellular Level: What Is the Leading Contributor?

P-glycoprotein interactions of novel psychoactive substances – Stimulation of ATP consumption and transport across Caco-2 monolayers

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