Asfour Marwa H, Mohsen Amira M
Pharmaceutical Technology Department, National Research Centre, El-Buhouth Street, Dokki, Cairo 12622, Egypt.
J Adv Res. 2017 Oct 12;9:17-26. doi: 10.1016/j.jare.2017.10.003. eCollection 2018 Jan.
The objective of this study was to target rutin, in a more solubilized form, to the colon aiming at treatment of colon carcinoma. pH sensitive nanospheres were prepared by the nanoprecipitation technique employing Eudragit S100. Different drug: polymer ratios as well as different concentrations of the stabilizer Poloxamer-188 were used. The developed rutin nanospheres exhibited entrapment efficiency ranging from 94.19% to 98.1%, with a zeta potential values <-20 mV. They were spherical in shape and their sizes were in the nanometric dimensions. The release study of nanospheres formulations revealed enhancement of aqueous solubility of rutin and indicated drug targeting to the colon. The selected formulations were stable after storage for 6 months at ambient room and refrigeration temperatures. cytotoxic study was conducted on human colon cancer (HCT-116) as well as normal human fibroblasts (BHK) cell lines, employing Sulphorhodamine-B assay. Rutin nanospheres showed significantly ( = .001) higher area under inhibition percentage curve, when compared to free drug, revealing more than 2-fold increase in rutin cytotoxic activity. These results reveal that Eudragit S100 nanospheres could be a potential drug delivery system to the colon with enhanced solubility and hence improved the cytotoxic activity of rutin.
本研究的目的是将更易溶解形式的芦丁靶向输送至结肠，以治疗结肠癌。采用Eudragit S100通过纳米沉淀技术制备了pH敏感纳米球。使用了不同的药物与聚合物比例以及不同浓度的稳定剂泊洛沙姆-188。所制备的芦丁纳米球的包封率在94.19%至98.1%之间，zeta电位值＜-20 mV。它们呈球形，尺寸在纳米范围内。纳米球制剂的释放研究表明芦丁的水溶性有所提高，并显示出药物对结肠的靶向性。所选制剂在室温和冷藏温度下储存6个月后仍保持稳定。采用磺酰罗丹明-B法对人结肠癌（HCT-116）以及正常人成纤维细胞（BHK）细胞系进行了细胞毒性研究。与游离药物相比，芦丁纳米球的抑制率曲线下面积显著更高（P = 0.001），表明芦丁的细胞毒性活性增加了两倍多。这些结果表明，Eudragit S100纳米球可能是一种潜在的结肠药物递送系统，具有增强的溶解性，从而提高了芦丁的细胞毒性活性。
