Department of Physical Chemistry, Faculty of Pharmacy, University of Barcelona, Joan XXIII Avenue, Barcelona 08028, Spain; Centro de Investigaciones Químicas, Universidad Autónoma del Estado de Morelos, Avenida de la Universidad 1001, Cuernavaca 62209, Morelos, Mexico.
Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Granada, Campus of Cartuja s/n, Granada 18071, Spain.
Colloids Surf B Biointerfaces. 2014 Apr 1;116:183-92. doi: 10.1016/j.colsurfb.2013.12.009. Epub 2014 Jan 6.
Many of the inflammatory diseases are becoming common in ageing society throughout the world. The clinically used anti-inflammatory drugs suffer from the disadvantage of side effects. Alternative to these drugs are natural products, since ancient times traditional medicines are being used for the treatment of inflammation. In the present study, four flavanones isolated from Eysenhardtia platycarpa leaves with a potent pharmacological activity were formulated in effective drug delivery systems: nanoemulsion and polymeric nanoparticles for topical use as novel anti-inflammatory topical formulations. Nanoemulsion system exhibited droplet sizes less than 70 nm and polymeric nanoparticles with a size of 156-202 nm possessed zeta potential values less than -25 mV that provided good stability and obtained high entrapment efficiency (78-90%). In vitro release and ex vivo permeation studies were performed on Franz-type diffusion cells and quantified by high performance liquid chromatography (HPLC), all formulations showed steady state release profiles over time and steady increase of flavanones in the skin permeation test. The anti-inflammatory activity, tested by TPA (12-O-tetradecanoylphorbol-13-acetate), induced oedema in mice ear suggesting that prenylated flavanones improve significantly their anti-inflammatory activity when are vehiculized in nanosized systems. Our results suggested that 5-hydroxy-7-methoxy-6-prenyl flavanone loaded nanoemulsion and polymeric nanoparticle could be proposed as potential topical anti-inflammatory formulations with the best properties for the treatment of inflammatory disorders.
许多炎症性疾病在全球老龄化社会中变得越来越普遍。临床上使用的抗炎药物存在副作用的缺点。这些药物的替代品是天然产物，因为自古以来传统药物就被用于治疗炎症。在本研究中，从扁核木(Eysenhardtia platycarpa)叶中分离出的四种具有强大药理活性的黄烷酮被制成有效的药物传递系统：纳米乳液和聚合物纳米粒，用于局部使用，作为新型抗炎局部制剂。纳米乳液系统的粒径小于 70nm，聚合物纳米粒的粒径为 156-202nm，具有小于-25mV 的 ζ 电位值，提供了良好的稳定性，并获得了高包封效率（78-90%）。在 Franz 型扩散细胞上进行了体外释放和离体渗透研究，并通过高效液相色谱法（HPLC）进行定量分析，所有制剂在一段时间内均显示出稳定的释放曲线，并在皮肤渗透试验中稳定增加了黄烷酮的含量。通过 TPA（12-O-十四烷酰佛波醇-13-乙酸酯）测试抗炎活性，在小鼠耳中诱导水肿，表明prenylated 黄烷酮在纳米化系统中运载时，其抗炎活性显著提高。我们的结果表明，负载 5-羟基-7-甲氧基-6-prenyl 黄烷酮的纳米乳液和聚合物纳米粒可被提议作为潜在的局部抗炎制剂，具有治疗炎症性疾病的最佳特性。
