Puerarin transport across a Calu-3 cell monolayer &amp;ndash;&amp;nbsp;an in vitro model of nasal mucosa permeability and the influence of paeoniflorin and menthol

Zhang, Lin; Du, Shouying; Lu, Yang; Liu, Chang; Tian, Zhihao; Chen, Yang; Wu, Huichao; Wang, Zhen

doi:10.2147/dddt.s110247

Cited by 27 publications

(17 citation statements)

References 44 publications

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“…The impact of aspirin absorption after PNS addition was investigated using our previously published method [ 37 ]. Briefly, Caco-2 cells were seeded at 2 × 10 5 cells/mL on the PET membranes in transwell chambers and allowed to form monolayers.…”

Section: Methodsmentioning

confidence: 99%

Inhibitory Influence of Panax notoginseng Saponins on Aspirin Hydrolysis in Human Intestinal Caco-2 Cells

Sun

Yang

et al. 2018

Molecules

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Herb-drug interactions are important safety concerns in clinical practice. The interactions occur firstly in the intestinal absorption for orally administered drugs. Aspirin and Panax notoginseng saponins (PNS)-based drugs are often combined in China to prevent larger-artery atherosclerosis. Here, we aimed to characterize the aspirin transport across Caco-2 cell monolayers, a model of the intestinal absorption, and further to evaluate the influence of PNS on aspirin hydrolysis and the relating mechanisms. Transcellular transport of aspirin and the influence of PNS were explored using Caco-2 cell monolayers. The protein expression of human carboxylesterase 1 (hCE1) and hCE2 in Caco-2 cells after PNS treatment was analyzed by ELISA, and the mRNA level were determined by qRT-PCR. In the study, Caco-2 cells showed high level of hydrolase activity, and most aspirin was hydrolyzed inside the cells during the transport process. Interestingly, PNS were demonstrated to inhibit the esterase activities responsible for aspirin hydrolysis in Caco-2 cells. PNS could also decrease the protein expression of hCE1 and hCE2, whereas exhibited minor effect on the mRNA expression. These results indicated that oral administration of PNS-based drugs might inhibit the hydrolysis of aspirin during intestinal absorption thus promoting its bioavailability.

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Section: Methodsmentioning

confidence: 99%

Inhibitory Influence of Panax notoginseng Saponins on Aspirin Hydrolysis in Human Intestinal Caco-2 Cells

Sun

Yang

et al. 2018

Molecules

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“…Some plant essential oils could act as promoters to enhance drug permeation through skin (Chen et al, ; Yi, Yan, Tang, Huang, & Kang, ), gastrointestinal mucous membrane (Xiao, Chen, Ping, & Chen, ), nasal mucosa (Zhang et al, ), cornea (Huang, Bai, Yang, Liu, & Cui, ; Qi et al, ), and BBB (Chen et al, ). In this article LIG, SENA, and SENI in chuanxiong volatile oil, increased the transport amount of ECH to different degrees, and the prompting effect of SENI was the strongest.…”

Section: Discussionmentioning

confidence: 99%

The influence and mechanism of ligustilide, senkyunolide I, and senkyunolide A on echinacoside transport through MDCK‐MDR1 cells as blood–brain barrier in vitro model

Zheng

Tang

et al. 2017

Phytotherapy Research

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Efficient transcytosis across the blood-brain-barrier is an important strategy for accessing drug targets within the central nervous system. Ligusticum chuanxiong Hort. was used as a messenger drug to increase the distribution of drugs in brain tissue in Traditional Chinese Medicine. The present study investigates the transport of echinacoside (ECH) through MDCK-MDR1 cell and the effects of ligustilide (LIG), senkyunolide A (SENA) and senkyunolide I (SENI) in chuanxiong on its transport. The results indicated that the absorption of ECH was relatively poor in MDCK-MDR1cells, and was concentration dependent and not saturable. The P-glycoprotein inhibitor verapamil could significantly increase the transport of ECH. It indicated that the transport mechanism might be passive diffusion as the dominating process with the active transportation mediated mechanism involved. The increased apparent permeability of ECH in A → B direction by ethylenediaminetetraacetic acid-Na suggested that ECH was absorbed via the paracellular route. The transport of ECH in A → B direction significantly increased when co-administrated with increasing concentrations of LIG, SENI and SENA. Western blot analysis and a decrease in transepithelial electrical resistance during the permeation experiment indicated that LIG, SENI and SENA had enhanced the transport of ECH in the BBB models attribute to down-regulate the expressions of claudin-5 and zonula occludens-1 expression.

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“… 10 , 11 In addition, we had chosen Calu-3 cells (derived from a human lung adenocarcinoma cell line) to model the nasal mucosa and to preliminarily evaluate the influence of puerarin in combination with peoniflorin and menthol on enhanced cell permeability. 12 The apparent permeability coefficients ( P app ) of puerarin bidirectional transport were both <1.5×10 −6 cm/s, and the efflux ratio (ER) was <1.5, indicating that puerarin alone exhibited poor absorption and that its transport primarily occurred by passive diffusion through the cell monolayer. When puerarin was coadministered with peoniflorin, the P app remained unaltered ( P >0.05).…”

Section: Introductionmentioning

confidence: 94%

Puerarin transport across rat nasal epithelial cells and the influence of compatibility with paeoniflorin and menthol

Zhang

et al. 2017

DDDT

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Nose-to-brain transport can provide an excellent pathway for drugs of the central nervous system. Consequently, how to make full use of this pathway in practical applications has become a focus of drug design. However, many aspects affecting drug delivery from the nose to the brain remain unclear. This study aimed to more deeply investigate the transport of puerarin and to explore the mechanism underlying the influence of compatible drugs on puerarin permeability in a primary cell model simulating the nasal mucosa. In this research, based on rat nasal epithelial cells (RNECs) cultured in vitro and cytotoxicity assays, the bidirectional transport of puerarin across RNEC monolayers and the effect of its compatibility with peoniflorin and menthol were analyzed. The apparent permeability coefficient was <1.5×10−6 cm/s, and the efflux ratio of puerarin was <2, indicating that puerarin had poor absorption and that menthol but not peoniflorin significantly improved puerarin transport. Simultaneously, through experiments, such as immunofluorescence staining, transepithelial electrical resistance measurement, rhodamine 123 efflux evaluation, the cell membrane fluorescence recovery after photobleaching test, and ATPase activity determination, the permeability promoting mechanism of menthol was confirmed to be closely related to disruption of the tight junction protein structure, to the P-glycoprotein inhibitory effect, to increased membrane fluidity, and to the promotion of enzyme activity. These results provide reliable data on nasal administration of the studied drugs and lay the foundation for a deeper investigation of the nose–brain pathway and nasal administration.

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Puerarin transport across a Calu-3 cell monolayer – an in vitro model of nasal mucosa permeability and the influence of paeoniflorin and menthol

Cited by 27 publications

References 44 publications

Inhibitory Influence of Panax notoginseng Saponins on Aspirin Hydrolysis in Human Intestinal Caco-2 Cells

Inhibitory Influence of Panax notoginseng Saponins on Aspirin Hydrolysis in Human Intestinal Caco-2 Cells

The influence and mechanism of ligustilide, senkyunolide I, and senkyunolide A on echinacoside transport through MDCK‐MDR1 cells as blood–brain barrier in vitro model

Puerarin transport across rat nasal epithelial cells and the influence of compatibility with paeoniflorin and menthol

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