PDF(Pubmed)
Abstract：
In this study, chitosan low molecular weight (LCH) and chitosan medium molecular weight (MCH) were employed to encapsulate a yarrow extract rich in chlorogenic acid and dicaffeoylquinic acids (DCQAs) that showed antiproliferative activity against colon adenocarcinoma cells. The design of CH micro/nanoparticles to increase the extract colon delivery was carried out by using two different techniques: ionic gelation and spray drying. Ionic gelation nanoparticles obtained were smaller and presented higher yields values than spray-drying microparticles, but spray-drying microparticles showed the best performance in terms of encapsulation efficiency (EE) (> 94%), also allowing the inclusion of a higher quantity of extract. Spray-drying microparticles designed using LCH with an LCH:extract ratio of 6:1 (1.25 mg/mL) showed a mean diameter of 1.31 ± 0.21 µm and EE values > 93%, for all phenolic compounds studied. The release profile of phenolic compounds included in this formulation, at gastrointestinal pHs (2 and 7.4), showed for most of them a small initial release, followed by an increase at 1 h, with a constant release up to 3 h. Chlorogenic acid presented the higher release values at 3 h (56.91% at pH 2; 44.45% at pH 7.4). DCQAs release at 3 h ranged between 9.01- 40.73%, being higher for 1,5- and 3,4-DCQAs. After gastrointestinal digestion, 67.65% of chlorogenic and most DCQAs remained encapsulated. Therefore, spray-drying microparticles can be proposed as a promising vehicle to increase the colon delivery of yarrow phenolics compounds (mainly chlorogenic acid and DCQAs) previously described as potential agents against colorectal cancer.
摘要：
在这项研究中,采用壳聚糖低分子量（LCH）和壳聚糖中分子量（MCH）封装富含绿原酸和二咖啡酰奎尼酸（DCQAs）的yarrow提取物，该提取物对结肠腺癌细胞具有抗增殖活性。通过使用两种不同的技术:离子凝胶化和喷雾干燥进行CH微米/纳米颗粒的设计以增加提取物结肠递送。获得的离子凝胶化纳米粒子比喷雾干燥微粒更小，并且具有更高的产率值，但喷雾干燥微粒在包封效率(EE)方面表现最佳(>94%)，还允许包含更大量的提取物。使用LCH设计的喷雾干燥微粒的LCH：提取物比例为6：1（1.25mg/mL），平均直径为1.31±0.21µm，EE值>93％，对于所有研究的酚类化合物。该制剂中包含的酚类化合物的释放曲线，在胃肠道pH值（2和7.4），向他们中的大多数展示了一个小的初始版本，随后在1小时增加，绿原酸在3小时时呈现较高的释放值(在pH2时为56.91%;在pH7.4时为44.45%)。3小时的DCQAs释放范围在9.01-40.73%之间，1,5-和3,4-DCQA更高。胃肠消化后，67.65%的绿原和大多数DCQAs保持包封。因此,可以提出喷雾干燥微粒作为一种有前途的载体,以增加先前描述为针对结肠直肠癌的潜在药剂的yarrow酚类化合物(主要是绿原酸和DCQAs)的结肠递送。
