Antihypertensive activity of spray-dried nanoemulsion containing Asiatic acid-Palm oil in high salt diet-fed rats

Pharmacia Pub Date : 2024-03-05 DOI:10.3897/pharmacia.71.e115091

A. Pradana, G. Ritthidej, Vudhiporn Limprasutr, Ausana Wongtayan, V. Lipipun, Iksen

{"title":"Antihypertensive activity of spray-dried nanoemulsion containing Asiatic acid-Palm oil in high salt diet-fed rats","authors":"A. Pradana, G. Ritthidej, Vudhiporn Limprasutr, Ausana Wongtayan, V. Lipipun, Iksen","doi":"10.3897/pharmacia.71.e115091","DOIUrl":null,"url":null,"abstract":"Asiatic acid (AA) is a compound isolated from Centella asiatica, which possesses significant antihypertensive activity. Several studies have shown that its hypertensive activity can be attributed to various mechanisms, such as Angiotensin-Converting-Enzyme (ACE) inhibition in the renin-angiotensin-aldosterone system (RAAS) pathway. Meanwhile, palm oil (PO) is an antioxidant, which has proven to have synergistic effects with the compound by preventing arterial thrombosis and atherosclerosis. Despite these synergistic effects, AA dosage in antihypertensive therapy has been reported to be relatively high compared to the common synthetic drug captopril. Therefore, this study aimed to produce spray-dried powder of nanoemulsion to enhance the solubility of AA, decrease the possibility of oxidation, and increase its activity. Redispersed AA nanoparticles were also successfully obtained during the synthesis process. Several evaluations were carried out, including particle size, particle distribution, zeta potential, cell viability, and antihypertensive activity in rats to ensure the improvement of physicochemical characteristics and activity as antihypertensive agent. The results showed that AA succeeded in forming nanoemulsion with excipients. In addition, it was encapsulated in a maltodextrin carrier, exhibiting good physicochemical characteristics and safety to the Caco-2 cells. The redispersion of the spray-dried powder yielded nanoparticles with a size of 217.4 ± 10.196 nm. The spray-dried nanoemulsion of AA also had faster effect than non-formulated AA (raw powder) in lowering the blood pressure of hypertensive Sprague-Dawley (SD) rats.\n Graphical abstract:\n \n \n","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2024-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmacia","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3897/pharmacia.71.e115091","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}

引用次数: 0

Abstract

Asiatic acid (AA) is a compound isolated from Centella asiatica, which possesses significant antihypertensive activity. Several studies have shown that its hypertensive activity can be attributed to various mechanisms, such as Angiotensin-Converting-Enzyme (ACE) inhibition in the renin-angiotensin-aldosterone system (RAAS) pathway. Meanwhile, palm oil (PO) is an antioxidant, which has proven to have synergistic effects with the compound by preventing arterial thrombosis and atherosclerosis. Despite these synergistic effects, AA dosage in antihypertensive therapy has been reported to be relatively high compared to the common synthetic drug captopril. Therefore, this study aimed to produce spray-dried powder of nanoemulsion to enhance the solubility of AA, decrease the possibility of oxidation, and increase its activity. Redispersed AA nanoparticles were also successfully obtained during the synthesis process. Several evaluations were carried out, including particle size, particle distribution, zeta potential, cell viability, and antihypertensive activity in rats to ensure the improvement of physicochemical characteristics and activity as antihypertensive agent. The results showed that AA succeeded in forming nanoemulsion with excipients. In addition, it was encapsulated in a maltodextrin carrier, exhibiting good physicochemical characteristics and safety to the Caco-2 cells. The redispersion of the spray-dried powder yielded nanoparticles with a size of 217.4 ± 10.196 nm. The spray-dried nanoemulsion of AA also had faster effect than non-formulated AA (raw powder) in lowering the blood pressure of hypertensive Sprague-Dawley (SD) rats. Graphical abstract:

查看原文本刊更多论文

含亚西亚酸-棕榈油的喷雾干燥纳米乳液对高盐饮食大鼠的抗高血压活性

积雪草酸（AA）是从积雪草中分离出来的一种化合物，具有显著的降压活性。多项研究表明，其高血压活性可归因于多种机制，如抑制肾素-血管紧张素-醛固酮系统（RAAS）途径中的血管紧张素转换酶（ACE）。同时，棕榈油（PO）是一种抗氧化剂，已被证明与该化合物具有协同作用，可防止动脉血栓形成和动脉粥样硬化。尽管有这些协同作用，但据报道，与常见的合成药物卡托普利相比，AA 在降压治疗中的用量相对较高。因此，本研究旨在生产纳米乳液喷雾干燥粉末，以提高 AA 的溶解度，降低氧化的可能性，并增加其活性。在合成过程中，还成功获得了再分散 AA 纳米粒子。研究人员进行了多项评估，包括粒度、粒度分布、ZETA电位、细胞存活率和大鼠降压活性，以确保改善 AA 的理化特性并提高其作为降压药的活性。结果表明，AA 成功地与辅料形成了纳米乳液。此外，它还被包裹在麦芽糊精载体中，显示出良好的理化特性和对 Caco-2 细胞的安全性。喷雾干燥粉末再分散后得到的纳米颗粒大小为 217.4 ± 10.196 nm。喷雾干燥的AA纳米乳液在降低高血压Sprague-Dawley（SD）大鼠血压方面的效果也比非制剂AA（原粉）更快。图表摘要：

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Pharmacia

自引率

0.00%

发文量