de Sá Coutinho Diego, Pires Jader, Gomes Hyago, Raffin Pohlmann Adriana, Stanisçuaski Guterres Sílvia, Rodrigues E Silva Patrícia Machado, Martins Marco Aurelio, Ferrarini Stela Regina, Bernardi Andressa
Laboratory of Inflammation, Oswaldo Cruz Institute, Oswaldo Cruz Foundation, Rio de Janeiro 21040-360, Brazil.
Institute of Health Sciences, Federal University of Mato Grosso, Sinop 78550-728, Brazil.
Pharmaceutics. 2020 Nov 11;12(11):1075. doi: 10.3390/pharmaceutics12111075.
Pequi is a Brazilian fruit used in folk medicine for pulmonary diseases treatment, but its oil presents bioavailability limitations. The use of nanocarriers can overcome this limitation. We developed nanoemulsions containing pequi oil (pequi-NE) and evaluated their effects in a lipopolysaccharide (LPS)-induced lung injury model. Free pequi oil or pequi-NE (20 mg/kg) was orally administered to A/J mice 16 and 4 h prior to intranasal LPS exposure, and the analyses were performed 24 h after LPS provocation. The physicochemical results revealed that pequi-NE comprised particles with mean diameter of 174-223 nm, low polydispersity index (0.11 ± 0.01), zeta potential of -7.13 ± 0.08 mV, and pH of 5.83 ± 0.12. In vivo evaluation showed that free pequi oil pretreatment reduced the influx of inflammatory cells into bronchoalveolar fluid (BALF), while pequi-NE completely abolished leukocyte accumulation. Moreover, pequi-NE, but not free pequi oil, reduced myeloperoxidase (MPO), TNF-α, IL-1β, IL-6, MCP-1, and KC levels. Similar anti-inflammatory effects were observed when LPS-exposed animals were pre-treated with the nanoemulsion containing pequi or oleic acid. These results suggest that the use of nanoemulsions as carriers enhances the anti-inflammatory properties of oleic acid-containing pequi oil. Moreover, pequi's beneficial effect is likely due its high levels of oleic acid.
佩基果是一种巴西水果,在民间医学中用于治疗肺部疾病,但其油的生物利用度存在局限性。使用纳米载体可以克服这一局限性。我们制备了含有佩基果油的纳米乳剂(佩基 - 纳米乳剂),并评估了它们在脂多糖(LPS)诱导的肺损伤模型中的作用。在鼻内暴露LPS前16小时和4小时,将游离佩基果油或佩基 - 纳米乳剂(20毫克/千克)口服给予A/J小鼠,并在LPS激发后24小时进行分析。物理化学结果显示,佩基 - 纳米乳剂由平均直径为174 - 223纳米、低多分散指数(0.11±0.01)、ζ电位为 - 7.13±0.08毫伏和pH值为5.83±0.12的颗粒组成。体内评估表明,游离佩基果油预处理减少了炎症细胞流入支气管肺泡灌洗液(BALF),而佩基 - 纳米乳剂完全消除了白细胞积聚。此外,佩基 - 纳米乳剂而非游离佩基果油降低了髓过氧化物酶(MPO)、肿瘤坏死因子 - α、白细胞介素 - 1β、白细胞介素 - 6、单核细胞趋化蛋白 - 1和KC水平。当用含有佩基果或油酸的纳米乳剂预处理LPS暴露的动物时,观察到类似的抗炎作用。这些结果表明,使用纳米乳剂作为载体可增强含油酸的佩基果油的抗炎特性。此外,佩基果的有益作用可能归因于其高含量的油酸。