Transport of curcumin derivatives in Caco-2 cell monolayers

Zeng, Zhen; Shen, Zhe L.; Zhai, Shuo; Xu, Jia; Liang, Hui; Shen, Qiang; Li, Qing Y.

doi:10.1016/j.ejpb.2017.04.004

Cited by 55 publications

(45 citation statements)

References 31 publications

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“…Our Caco‐2 monolayers grown for 21 days developed a suitable absorptive barrier, as evidenced by the high TEER values, the absence of LY leakage (i.e. high integrity of tight junction complex) and the presence of P‐gp activity …”

Section: Discussionmentioning

confidence: 95%

“…high integrity of tight junction complex) and the presence of P-gp activity. [20,21,23,31] The hydrophilic LY moves across the cell monolayers only via the paracellular route. [21,22,32] Thus, LY flux across the monolayers increases when the tight junction is loosened.…”

Section: Discussionmentioning

confidence: 99%

“…TEER was measured with the use of a chopstick‐like electrode connected to a Millicell‐ERS ® (electrical resistance system; Millipore Corporation, Bedford, MA, USA). Only monolayers having TEER values above 300 Ω/cm 2 were used for the transport experiments . TEER was measured both before and at the end of the transport experiment.…”

Section: Methodsmentioning

confidence: 99%

“…Only monolayers having TEER values above 300 O/cm 2 were used for the transport experiments. [18][19][20] TEER was measured both before and at the end of the transport experiment.…”

Section: Caco-2 Cell Monolayer Integrity Testsmentioning

confidence: 99%

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Potential P-glycoprotein-mediated herb-drug interaction of phyllanthin at the intestinal absorptive barrier

Dunkoksung

Vardhanabhuti

Jianmongkol

2018

Journal of Pharmacy and Pharmacology

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Objectives This study investigated the absorptive potential of phyllanthin across the polarized Caco‐2 monolayers and the potential role of phyllanthin in P‐glycoprotein (P‐gp)‐mediated drug interaction. Methods The absorptive potential of phyllanthin was predicted from its apparent permeability (Papp) across the Caco‐2 monolayers under the pH gradient condition (pH 6.5AP–7.4BL) at 37°C. Integrity of paracellular transport was assessed by monitoring transepithelial electrical resistance (TEER) and lucifer yellow (LY) leakage. P‐gp‐mediated interaction was evaluated by transport studies of phyllanthin and rhodamine‐123. Key findings The absorptive Papp of phyllanthin (34.90 ± 1.18 × 10−6 cm/s) was in the same rank order as the high permeable theophylline and antipyrine. Phyllanthin transport in the absorptive and secretive directions was comparable (the efflux ratio (ER) of 1.19 ± 0.01). Phyllanthin caused no changes in TEER nor LY leakage in the monolayers. However, phyllanthin increased rhodamine‐123 ER in a concentration‐dependent manner, suggesting its inhibition on P‐gp function. In addition, phyllanthin aqueous solubility was <5 μg/ml at 37°C. Conclusions Phyllanthin is a highly permeable compound that could passively diffuse through the absorptive barrier via transcellular pathway with little hindrance from P‐gp. Phyllanthin could interfere with transport of P‐gp drug substrates, when concomitantly administered. In addition, aqueous solubility could be a limiting factor in phyllanthin absorption.

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Section: Discussionmentioning

confidence: 95%

Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

“…Only monolayers having TEER values above 300 O/cm 2 were used for the transport experiments. [18][19][20] TEER was measured both before and at the end of the transport experiment.…”

Section: Caco-2 Cell Monolayer Integrity Testsmentioning

confidence: 99%

See 2 more Smart Citations

Potential P-glycoprotein-mediated herb-drug interaction of phyllanthin at the intestinal absorptive barrier

Dunkoksung

Vardhanabhuti

Jianmongkol

2018

Journal of Pharmacy and Pharmacology

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“…96 Another study investigating ferulic acidloaded SLNs against neurotoxicity found that ferulic acid can be extensively delivered to brain cells and can thereby prevent oxidation without any toxicity. 103 Curcumin is another potential compound that showed excellent anti-Alzheimeric effect in various in vitro and in vivo studies, [104][105][106][107][108][109][110][111][112] but it showed limitations in its bioavailability through oral delivery with a very low content in the brain, and could not achieve a significant potential effect. Therefore, many recent studies were intended to improve the bioavailability of curcumin to the brain through oral delivery via SLNs.…”

Section: Anti-alzheimer's Effectmentioning

confidence: 99%

Recent developments in solid lipid nanoparticle and surface-modified solid lipid nanoparticle delivery systems for oral delivery of phyto-bioactive compounds in various chronic diseases

Ganesan

Ramalingam

Karthivashan

et al. 2018

IJN

127

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Solid lipid nanoparticle (SLN) delivery systems have a wide applicability in the delivery of phyto-bioactive compounds to treat various chronic diseases, including diabetes, cancer, obesity and neurodegenerative diseases. The multiple benefits of SLN delivery include improved stability, smaller particle size, leaching prevention and enhanced lymphatic uptake of the bioactive compounds through oral delivery. However, the burst release makes the SLN delivery systems inadequate for the oral delivery of various phyto-bioactive compounds that can treat such chronic diseases. Recently, the surface-modified SLN (SMSLN) was observed to overcome this limitation for oral delivery of phyto-bioactive compounds, and there is growing evidence of an enhanced uptake of curcumin delivered orally via SMSLNs in the brain. This review focuses on different SLN and SMSLN systems that are useful for oral delivery of phyto-bioactive compounds to treat various chronic diseases.

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Uptake and time‐dependent subcellular localization of native and micellar curcumin in intestinal cells

2022

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Uptake into intestinal cells and intracellular distribution into metabolically competent organelles, such as the endoplasmic reticulum, are important processes potentially limiting the bioavailability of xenobiotics. The incorporation of curcumin into polysorbate 80 micelles improves its naturally low oral bioavailability in humans. Here, we investigated uptake and time‐dependent localization of curcumin in intestinal cells when administered as native or micellar formulation. Differentiated Caco‐2 cells were incubated with 200 μmol/L native or micellar curcumin for up to 180 min and cellular uptake was quantified. Intracellular curcumin was detected already after 30 min and did not differ significantly between formulations or over time. Subcellular localization of native and micellar curcumin in Caco‐2 cells was studied by density gradient centrifugation. After 30 min, curcumin from both formulations was mainly associated with mitochondria and lysosomes, after 180 min native curcumin was associated with mitochondria and peroxisomes, micellar curcumin with peroxisomes only. Uptake and localization of native and micellar curcumin in intestinal cells do not differ significantly and consequently do not explain differences in bioavailability in humans. The temporary co‐localization with lysosomes is in agreement with the previously proposed role of endocytosis in cellular uptake of curcumin and warrants further investigation.

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Transport of curcumin derivatives in Caco-2 cell monolayers

Cited by 55 publications

References 31 publications

Potential P-glycoprotein-mediated herb-drug interaction of phyllanthin at the intestinal absorptive barrier

Potential P-glycoprotein-mediated herb-drug interaction of phyllanthin at the intestinal absorptive barrier

Recent developments in solid lipid nanoparticle and surface-modified solid lipid nanoparticle delivery systems for oral delivery of phyto-bioactive compounds in various chronic diseases

Uptake and time‐dependent subcellular localization of native and micellar curcumin in intestinal cells

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