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首页> 外文期刊>Artificial cells, nanomedicine, and biotechnology. >Intranasal delivery of quercetin-loaded mucoadhesive nanoemulsion for treatment of cerebral ischaemia
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Intranasal delivery of quercetin-loaded mucoadhesive nanoemulsion for treatment of cerebral ischaemia

机译：槲皮素负载的粘膜粘附纳米乳剂的鼻内给药治疗脑缺血

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Abstract Background: Quercetin (QUR), as an antioxidant flavonoid, exhibits potential role in the amelioration of cerebral ischaemia; however, poor solubility as well as oral absorption results low serum and tissue levels for this drug. Purpose of the study: To enhance bioavailability, this study aims to prepare QUR nanoemulsions and administer via non-invasive nasal route in order to evaluate the drug targeting in brain. Methods: Quercetin mucoadhesive nanoemulsion (QMNE) was prepared (ionic gelation method) and optimized using various parameters, that is, particle size, entrapment efficiency, zeta potential and ex vivo permeation study. Results: The results observed for optimized QMNE were as follows: mean globule size (91.63?±?4.36?nm), zeta potential (?17.26?±?1.04?mV), drug content (99.84?±?0.34%) and viscosity (121?±?13?cp). To evaluate the extent of bioavailability for QMNE via post-intranasal (i.n.) administration, Ultra performance liquid chromatography-mass spectroscopy (UPLC-ESI-Q-TOF-MS/MS)-based bioanalytical method was developed and validated for pharmacokinetics, biodistribution, brain-targeting efficiency (9333.33?±?39.39%) and brain drug-targeting potential (2181.83?±?5.69%) which revealed enhanced QUR brain bioavailability as compared to intravenous administration (i.v.). Furthermore, improved neurobehavioral activity (locomotor and grip strength), histopathology and reduced infarction volume effects were observed in middle cerebral artery occlusion (MCAO)–induced cerebral ischemic rats model after i.n. administration of QMNE. Conclusion: This study supports a significant role for QMNE in terms of high brain-targeting potential and formulation efficiency due to ease of access and effective targeting in brain.
机译：摘要背景：槲皮素（QUR）是一种抗氧化剂类黄酮，在改善脑缺血方面具有潜在作用。但是，该药物溶解性差以及口服吸收不良，导致血清和组织水平降低。研究目的：为了提高生物利用度，本研究旨在制备QUR纳米乳剂并通过无创鼻腔途径给药，以评估脑部靶向药物。方法：制备槲皮素粘膜粘附纳米乳剂（离子凝胶法），并使用各种参数进行优化，包括粒径，包封率，ζ电位和离体渗透研究。结果：对优化的QMNE观察到的结果如下：平均小球尺寸（91.63≤±4.36μm），ζ电位（≤17.26≤±1.04μmV），药物含量（99.84≤±0.34％）和粘度（121±±13℃）。为了评估经鼻内给药的QMNE的生物利用度，开发了基于超高效液相色谱-质谱（UPLC-ESI-Q-TOF-MS / MS）的生物分析方法，并验证了其药代动力学，生物分布，与静脉给药相比，脑靶向效率（9333.33±39.39％）和脑药物靶向潜力（2181.83±±5.69％）显示出QUR脑生物利用度的提高。此外，在i.n.之后，在大脑中动脉闭塞（MCAO）诱发的脑缺血大鼠模型中，观察到神经行为活动（运动能力和握力）的改善，组织病理学和梗死体积的减少。 QMNE的管理。结论：由于易于接近和有效靶向大脑，该研究支持QMNE在高大脑靶向潜力和制剂效率方面的重要作用。

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