Itraconazole (ITR), an antifungal agent has poor bioavailability due to low aqueous solubility. The present investigation aimed at development of ITR nanoemulsion to enhance its oral bioavailability. ITR nanoemulsion was prepared using Capmul MCM C8 as oil, Pluronic F68 as co-surfactant and Cremophore EL as surfactant using high speed stirring, followed by probe sonication. Nanoemulsion with average globule size of 100.9 nm and zeta potential of -35.9 ± 1.2 mV was able to penetrate well into the intestinal membrane as confirmed by the laser confocal scanning microscopy and ex vivo intestinal permeability study. Antimycotic study confirmed the efficacy of ITR nanoemulsion. Significantly higher values of pharmacokinetic parameters the formulation than the plain drug and marketed formulation indicated an increase in the bioavailability of ITR. The prepared nanoemulsion was stable at both, refrigerated and room temperature conditions. Nanoemulsion of ITR seems to be a promising formulation for enhancement of its oral bioavailability.

中文翻译：

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伊曲康唑纳米乳增强口服生物利用度的配制和评价。


伊曲康唑（ITR）是一种抗真菌剂，由于水溶性低，生物利用度差。本研究旨在开发 ITR 纳米乳剂以提高其口服生物利用度。使用 Capmul MCM C8 作为油、Pluronic F68 作为助表面活性剂、Cremophore EL 作为表面活性剂，使用高速搅拌，然后进行探针超声处理，制备 ITR 纳米乳液。激光共聚焦扫描显微镜和离体肠道通透性研究证实，平均小球尺寸为 100.9 nm、zeta 电位为 -35.9 ± 1.2 mV 的纳米乳液能够很好地渗透到肠膜中。抗真菌研究证实了ITR纳米乳的功效。该制剂的药代动力学参数值显着高于普通药物和市售制剂，表明 ITR 的生物利用度有所增加。制备的纳米乳液在冷藏和室温条件下均稳定。 ITR 纳米乳剂似乎是一种有前景的增强口服生物利用度的制剂。