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首页> 美国卫生研究院文献>Drug Design Development and Therapy >Puerarin transport across a Calu-3 cell monolayer – an in vitro model of nasal mucosa permeability and the influence of paeoniflorin and menthol
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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

机译：葛根素跨Calu-3细胞单层转运-鼻粘膜通透性的体外模型以及pa药苷和薄荷醇的影响

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摘要

Nasal administration is a high-potential delivery system, particularly because it can provide a pathway from the nose to the brain. The objective of this research is to characterize puerarin transport across a Calu-3 cell monolayer used as a model of the nasal mucosa and to evaluate the influence of puerarin in combination with paeoniflorin and menthol to explore the enhanced mechanism of the permeability at the cell level. The apparent permeability coefficients (Papp) of puerarin bidirectional transport were both <1.5×10−6 cm/s, and the efflux ratio 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 coad ministered with paeoniflorin, the Papp was not changed (P>0.05). However, the addition of menthol significantly (P<0.05) improved the Papp of puerarin in both directions. Moreover, based on immunofluorescence experiments and transepithelial electrical resistance measurements, the data indicated that the drug compatibility opened tight junctions and weakened the barrier capabilities of epithelial cells, thereby promoting the permeability of puerarin.
机译：鼻腔给药是一种高潜力的给药系统，特别是因为它可以提供从鼻子到大脑的途径。这项研究的目的是表征葛根素跨Calu-3细胞单层作为鼻粘膜模型的转运，并评估葛根素联合pa药苷和薄荷醇的影响，以探索细胞水平通透性的增强机制。 。葛根素双向传输的表观渗透系数（Papp）均<1.5×10 -6 cm / s，流出比<1.5，表明葛根素单独表现出较弱的吸收性，且其传输主要是通过细胞单层的被动扩散而发生。葛根素与pa药苷配伍后，P​​app值不变（P> 0.05）。然而，薄荷醇的添加显着（P <0.05）改善了葛根素在两个方向上的Papp。此外，基于免疫荧光实验和跨上皮电阻测量，数据表明药物相容性打开了紧密的连接并削弱了上皮细胞的屏障能力，从而促进了葛根素的通透性。

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