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棒状壳聚糖-喹啉纳米粒子的制备及表征作为 pH 响应型纳米载体用于槲皮素递送

Preparation and characterization of rod-like chitosan-quinoline nanoparticles as pH-responsive nanocarriers for quercetin delivery.

机构信息

School of Chemistry, College of Science, University of Tehran, PO Box 14155 6455, Tehran, Iran.

School of Chemistry, College of Science, University of Tehran, PO Box 14155 6455, Tehran, Iran.

出版信息

Int J Biol Macromol. 2019 May 1;128:279-289. doi: 10.1016/j.ijbiomac.2019.01.137. Epub 2019 Jan 26.

DOI:10.1016/j.ijbiomac.2019.01.137
PMID:30695722
Abstract

Novel chitosan-quinoline nanoparticles as anticancer drug nanocarriers were prepared using 2-chloro-3-formylquinoline and 3-formylquinolin-2(1H)-one as non-toxic modifying agents via oil-in-water nanoemulsion technique. Chitosan-quinoline nanoparticles were characterized by FT-IR, UV-vis spectrophotometry, XRD, SEM, AFM and DLS techniques. The morphological and particle size studies demonstrated that drug-loaded chitosan-quinoline nanoparticles have a regular nanorod shape and monolithic structure with the desired particle size of 141 to 174.8 nm and a negative zeta potential of -2.4 to -14.1 mV. Drug loading capacity (LC) and encapsulation efficiency (EE) were achieved using quercetin as a hydrophobic anticancer drug and were about 4.8-9.6% and 65.8-77%, respectively. The in vitro release studies displayed great pH-sensitive release behavior. Evaluation of the anticancer efficacy of quercetin loaded chitosan-quinoline nanoparticles using the in vitro cytotoxicity studies against HeLa cells indicated that the chitosan nanoparticles are a promising candidate for the anticancer drugs delivery.

摘要

采用 2-氯-3-甲酰基喹啉和 3-甲酰基喹啉-2(1H)-酮作为无毒修饰剂,通过油包水纳米乳液技术制备了新型壳聚糖-喹啉纳米粒子作为抗癌药物纳米载体。通过傅里叶变换红外光谱(FT-IR)、紫外可见分光光度法、X 射线衍射(XRD)、扫描电子显微镜(SEM)、原子力显微镜(AFM)和动态光散射(DLS)技术对壳聚糖-喹啉纳米粒子进行了表征。形态和粒径研究表明,载药壳聚糖-喹啉纳米粒子具有规则的纳米棒形状和整体结构,所需粒径为 141 至 174.8nm,且具有-2.4 至-14.1mV 的负 zeta 电位。使用山奈酚作为疏水性抗癌药物,通过测定载药量(LC)和包封效率(EE),分别达到了 4.8-9.6%和 65.8-77%。体外释放研究显示出良好的 pH 敏感性释放行为。通过体外细胞毒性研究对载有山奈酚的壳聚糖-喹啉纳米粒子的抗癌功效进行评估,结果表明壳聚糖纳米粒子是一种很有前途的抗癌药物递送候选物。

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