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Preparation and Evaluation of Novel Emodin-loaded Stearic Acid-g-chitosan Oligosaccharide Nanomicelles.
Nanoscale Research Letters ( IF 5.418 ) Pub Date : 2020-04-25 , DOI: 10.1186/s11671-020-03304-1
Xiaohong Jiang 1 , Mingxing Ma 2 , Mingjuan Li 1 , Shihong Shao 3 , Hong Yuan 3 , Fuqiang Hu 3 , Jianwen Liu 4 , Xuan Huang 1
Affiliation  

The purpose of this study was to prepare and characterize emodin-loaded stearic acid-g-chitosan oligosaccharide (CSO-SA/EMO) and to evaluate its antitumor activity in vitro. In this study, stearic acid-g-chitosan oligosaccharide was used as a carrier and its physicochemical properties were determined by different methods. Cell uptake behavior was examined using FITC-labeled stearic acid-g-chitosan oligosaccharide. CSO-SA/EMO was prepared using ultrasonication and dialysis. Particle size, surface potential, entrapment efficiency, and drug release behavior were studied in vitro. The effects of CSO-SA/EMO on gastric cancer cells were investigated using MTT assay and flow cytometry. Results showed CSO-SA/EMO particle size was larger and potential was smaller than that of stearic acid-g-chitosan oligosaccharide. The 12 h micellar uptake by MGC803 and BGC823 cells was sufficient, and the micelles were able to abundantly accumulate at lesion sites in mice thus achieving good passive EPR targeting. MTT and cell cycle arrest assays showed CSO-SA/EMO-enhanced antitumor activity significantly towards MGC803 and BGC823 cells compared with that of free emodine. Tumor volume, hematoxylin and eosin staining, and terminal deoxynucleotide transferase dUTP nick-end labeling assay proved CSO-SA/EMO had a significant antitumor effect on tumor tissues in vivo. In conclusion, the ultrasonication-dialysis method provided a simple and effective method for preparing CSO-SA/EMO. The delivery of emodine using a micelle system improved its antitumor effects effectively.

中文翻译:

新型硬脂酸-g-壳寡糖纳米胶束的制备与评价。

本研究的目的是制备和表征负载大黄素的硬脂酸-g-壳寡糖(CSO-SA/EMO)并评估其体外抗肿瘤活性。本研究以硬脂酸-g-壳寡糖为载体,通过不同方法测定其理化性质。使用 FITC 标记的硬脂酸-g-壳寡糖检查细胞摄取行为。CSO-SA/EMO 通过超声处理和透析制备。在体外研究了粒径、表面电位、包封效率和药物释放行为。采用MTT法和流式细胞术研究CSO-SA/EMO对胃癌细胞的影响。结果表明,与硬脂酸-g-壳寡糖相比,CSO-SA/EMO粒径较大,电位较小。MGC803和BGC823细胞12小时的胶束摄取是足够的,并且胶束能够在小鼠的病变部位大量积累,从而实现良好的被动EPR靶向。MTT 和细胞周期阻滞测定显示,与游离大黄素相比,CSO-SA/EMO 对 MGC803 和 BGC823 细胞的抗肿瘤活性显着增强。肿瘤体积、苏木精和伊红染色以及末端脱氧核苷酸转移酶dUTP缺口末端标记测定证明CSO-SA/EMO对体内肿瘤组织具有显着的抗肿瘤作用。总之,超声透析法为制备CSO-SA/EMO提供了一种简单有效的方法。利用胶束系统递送大黄素,有效提高了其​​抗肿瘤效果。
更新日期:2020-04-25
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