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Self-Nanoemulsifying Drug Delivery Systems Containing Plantago lanceolata—An Assessment of Their Antioxidant and Antiinflammatory Effects

机译:包含车前草的自纳米乳化药物递送系统-抗氧化和抗炎作用的评估

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摘要

The most important components of Plantago lanceolata L. leaves are catalpol, aucubin, and acteoside (=verbascoside). These bioactive compounds possess different pharmacological effects: anti-inflammatory, antioxidant, antineoplastic, and hepatoprotective. The aim of this study was to protect Plantago lanceolata extract from hydrolysis and to improve its antioxidant effect using self-nano-emulsifying drug delivery systems (SNEDDS). Eight SNEDDS compositions were prepared, and their physical properties, in vitro cytotoxicity, and in vivo AST/ALT values were investigated. MTT cell viability assay was performed on Caco-2 cells. The well-diluted samples (200 to 1000-fold dilutions) proved to be non-cytotoxic. The acute administration of PL-SNEDDS compositions resulted in minor changes in hepatic markers (AST, ALT), except for compositions >4 and >8 due to their high Transcutol contents (80%). The non-toxic compositions showed a significant increase in free radical scavenger activity measured by the DPPH test compared to the blank SNEDDS. An indirect dissolution test was performed, based on the result of the DPPH antioxidant assay; the dissolution profiles of Plantago lancolata extract were statistically different from each SNEDDS. The anti-inflammatory effect of PL-SNEDDS compositions was confirmed by the ear inflammation test. For the complete examination period, all compositions decreased ear edema as compared to the positive (untreated) control. It can be concluded that PL-SNEDDS compositions could be used to deliver active natural compounds in a stable, efficient, and safe manner.
机译:车前草叶的最重要成分是梓醇,aucubin和acteoside(= verbascoside)。这些生物活性化合物具有不同的药理作用:抗炎,抗氧化,抗肿瘤和保肝。这项研究的目的是使用自动纳米乳化药物递送系统(SNEDDS)保护车前草提取物免于水解,并提高其抗氧化作用。制备了八种SNEDDS组合物,并研究了它们的物理性质,体外细胞毒性和体内AST / ALT值。在Caco-2细胞上进行了MTT细胞活力测定。稀释良好的样品(稀释200至1000倍)被证明是无细胞毒性的。急性施用PL-SNEDDS组合物会导致肝脏标志物(AST,ALT)的微小变化,但组合物> 4 和> 8 由于其Transcutol含量高(80% )。与空白的SNEDDS相比,通过DPPH测试测得的无毒组合物自由基清除剂活性显着提高。根据DPPH抗氧化剂测定的结果进行了间接溶出度测试;车前子提取物的溶出曲线与每个SNEDDS都有统计学差异。 PL-SNEDDS组合物的抗炎作用通过耳部炎症试验得到证实。在整个检查期间,与阳性(未处理)对照相比,所有组合物均降低了耳部水肿。可以得出结论,PL-SNEDDS组合物可用于以稳定,有效和安全的方式递送活性天然化合物。

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