Subramanian Balajikarthick, Kuo Fonghsu, Ada Earl, Kotyla Tim, Wilson Thomas, Yoganathan Subbiah, Nicolosi Robert
Center for Health and Disease Research, University of Massachusetts, Lowell, MA 01854, USA.
Int Immunopharmacol. 2008 Nov;8(11):1533-9. doi: 10.1016/j.intimp.2008.06.009. Epub 2008 Jul 14.
Aspirin, a non-steroidal anti-inflammatory drug, widely used for its anti-inflammatory properties is associated with several systemic side effects including gastro-intestinal discomfort. Inflammation can be mediated by pro-inflammatory cytokines and, along with various other host factors eventually give rise to edema at the inflamed site. Because of the adverse side effects oftentimes associated with systemic exposure to aspirin, the aim of the present study was to investigate whether the anti-inflammatory property of aspirin would enhance if delivered as nano-emulsion preparation. Nano-emulsion preparations of aspirin prepared with a Microfluidizer Processor were evaluated in the croton-oil-induced ear edema CD-1 mouse model using ear lobe thickness and the accumulation of specific in situ cytokines as biomarkers of inflammation. The results showed that particle size (90 nm) populations of nano-emulsion preparations of aspirin compared to an aspirin suspension (363 nm), significantly decreased (p<0. 05) ear lobe thickness approximately 2 fold greater than the aspirin suspension. In addition, the aspirin nano-emulsion further reduced the auricular levels of IL-1alpha (-37%) and TNFalpha (-69%) compared to the aspirin suspension preparation (p<0.05). The reductions in ear lobe thickness were also significantly associated with accumulated tissue levels of IL-1alpha (r=0.5, p<0.009) and TNFalpha (r=0.7, p<0.0004), respectively. In conclusion, these studies indicate that a nano-emulsion preparation of aspirin significantly improved the anti-inflammatory properties of an aspirin suspension in a CD-1 mouse model of induced inflammation.
阿司匹林是一种非甾体抗炎药，因其抗炎特性而被广泛使用，但它会引发包括胃肠道不适在内的多种全身性副作用。炎症可由促炎细胞因子介导，并且与各种其他宿主因素一起最终导致炎症部位出现水肿。由于全身性使用阿司匹林时常会产生不良副作用，本研究的目的是调查如果将阿司匹林制成纳米乳剂制剂，其抗炎特性是否会增强。使用耳垂厚度以及特定原位细胞因子的积累作为炎症生物标志物，在巴豆油诱导的耳部水肿CD-1小鼠模型中评估了用微流控处理器制备的阿司匹林纳米乳剂制剂。结果表明，与阿司匹林悬浮液（363 nm）相比，阿司匹林纳米乳剂制剂的粒径（90 nm）群体显著降低（p<0.05），耳垂厚度比阿司匹林悬浮液大约减少了2倍。此外，与阿司匹林悬浮液制剂相比，阿司匹林纳米乳剂进一步降低了耳部IL-1α（-37%）和TNFα（-69%）的水平（p<0.05）。耳垂厚度的降低也分别与IL-1α（r=0.5，p<0.009）和TNFα（r=0.7，p<0.0004）的组织积累水平显著相关。总之，这些研究表明，在诱导炎症的CD-1小鼠模型中，阿司匹林纳米乳剂制剂显著改善了阿司匹林悬浮液的抗炎特性。
