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首页> 美国卫生研究院文献>Drug Design Development and Therapy >Puerarin transport across rat nasal epithelial cells and the influence of compatibility with peoniflorin and menthol
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Puerarin transport across rat nasal epithelial cells and the influence of compatibility with peoniflorin and menthol

机译：葛根素在大鼠鼻上皮细胞中的转运及其与药和薄荷醇的相容性的影响

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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.
机译：鼻子到大脑的运输可以为中枢神经系统的药物提供极好的途径。因此，如何在实际应用中充分利用这一途径已成为药物设计的重点。但是，影响从鼻子到大脑的药物输送的许多方面仍不清楚。这项研究旨在更深入地研究葛根素的运输，并在模拟鼻粘膜的原代细胞模型中探索相容药物对葛根素通透性的影响的潜在机制。在这项研究中，基于体外培养的大鼠鼻上皮细胞（RNEC）和细胞毒性测定，分析了葛根素跨RNEC单层的双向转运及其与with药和薄荷醇的相容性的影响。表观渗透系数为<1.5×10 −6 cm / s，葛根素的外排率为<2，表明葛根素的吸收较弱，薄荷醇而不是oni药苷明显改善了葛根素的转运。同时，通过免疫荧光染色，经上皮电阻测量，若丹明123流出评估，光漂白试验后细胞膜荧光恢复以及ATPase活性测定等实验，证实薄荷醇的通透性促进机制与破坏其密切相关。紧密连接的蛋白质结构，对P-糖蛋白有抑制作用，能增加膜的流动性，并能促进酶的活性。这些结果为研究药物的鼻腔给药提供了可靠的数据，并为深入研究鼻-脑途径和鼻腔给药奠定了基础。

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