Chaiittianan Rungsiri, Sripanidkulchai Bungorn
Center for Research and Development of Herbal Health Products, Faculty of Pharmaceutical Sciences, Khon Kaen University , Khon Kaen , Thailand.
Drug Dev Ind Pharm. 2014 Dec;40(12):1597-606. doi: 10.3109/03639045.2013.838580. Epub 2013 Sep 20.
For potential topical administration, we formulated a nanoemulsion containing phenolic constituents of Phyllanthus emblica branch extract. The nanoemulsion has high entrapment efficiency, small particle size, is stable, and can release its main chemical components. Branches of P. emblica were extracted with 50% ethanol (EPE) with 5.4% yield. HPLC analysis indicated several phenolic compounds, including gallic acid, vanillic acid, epigallocatechin (EGC), epigallocatechin gallate (EGCG) and ellagic acid. These were selected as chemical markers of EPE in the nanoemulsion development. The nanoemulsion was prepared by microemulsion techniques with hot high pressure homogenization. A ternary phase diagram was constructed to obtain the optimized nanoemulsion. The obtained transparent EPE nanoemulsion is composed of isopropyl myristate (0.6% w/w), Brij® 78 (0.35% w/w), and 0.15% (w/w) EPE. The optimized EPE nanoemulsion had a median particle size of 191.63 ± 4.07 nm with a narrow particle size distribution, a zeta potential of -10.19 ± 0.54 mV, high entrapment efficiency at 67.99 ± 0.87% and good stability at 4 °C after 90 d of storage. The release of active ingredients from the EPE nanoemulsion was slower than that of the EPE aqueous formulation. The loading ratios of the five phenolic compounds were high, with relative order of EGC > EGCG > vanillic acid > gallic acid > ellagic acid, resulting in slow release profiles of EGC and EGCG in the EPE nanoemulsion. In conclusion, the obtained EPE nanoemulsion has good characteristics for future clinical trials.
对于潜在的局部给药,我们制备了一种含有余甘子树枝提取物酚类成分的纳米乳剂。该纳米乳剂具有高包封率、小粒径、稳定性好且能释放其主要化学成分的特点。余甘子树枝用50%乙醇提取(EPE),得率为5.4%。高效液相色谱分析表明含有几种酚类化合物,包括没食子酸、香草酸、表没食子儿茶素(EGC)、表没食子儿茶素没食子酸酯(EGCG)和鞣花酸。这些被选为纳米乳剂开发中EPE的化学标志物。纳米乳剂采用微乳技术结合热高压均质法制备。构建三元相图以获得优化的纳米乳剂。所得透明的EPE纳米乳剂由肉豆蔻酸异丙酯(0.6% w/w)、Brij® 78(0.35% w/w)和0.15%(w/w)EPE组成。优化后的EPE纳米乳剂中位粒径为191.63±4.07 nm,粒径分布窄,ζ电位为-10.19±0.54 mV,包封率高,为67.99±0.87%,在4℃储存90天后稳定性良好。EPE纳米乳剂中活性成分的释放比EPE水性制剂慢。五种酚类化合物的负载率较高,相对顺序为EGC>EGCG>香草酸>没食子酸>鞣花酸,导致EPE纳米乳剂中EGC和EGCG的释放曲线较平缓。总之,所得EPE纳米乳剂具有良好的特性,可用于未来的临床试验。