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基于 pH 敏感的生物相容性壳聚糖/海泡石交联柠檬酸磁性纳米载体用于高效释放舒尼替尼。

pH-sensitive biocompatible chitosan/sepiolite-based cross-linked citric acid magnetic nanocarrier for efficient sunitinib release.

机构信息

Polymer Research Laboratory, Department of Organic and Biochemistry, Faculty of Chemistry, University of Tabriz, P.O. Box 51666, Tabriz, Iran.

Polymer Research Laboratory, Department of Organic and Biochemistry, Faculty of Chemistry, University of Tabriz, P.O. Box 51666, Tabriz, Iran; Research Center for Pharmaceutical Nanotechnology, Biomedicine Institute, Tabriz University of Medical Sciences, Tabriz, Iran.

出版信息

Int J Biol Macromol. 2023 Jul 1;242(Pt 1):124739. doi: 10.1016/j.ijbiomac.2023.124739. Epub 2023 May 5.

DOI:10.1016/j.ijbiomac.2023.124739
PMID:37148933
Abstract

In this study, the magnetite nanoparticles were immobilized on the sepiolite needles via co-precipitation of iron ions. Then, the resulted magnetic sepiolite (mSep) nanoparticles were coated with chitosan biopolymer (Chito) in the presence of citric acid (CA) to prepare mSep@Chito core-shell drug nanocarriers (NCs). TEM images showed magnetic FeO nanoparticles with small sizes (less than 25 nm) on the sepiolite needles. Sunitinib anticancer drug loading efficiencies were ⁓45 and 83.7 % for the NCs with low and high content of Chito, respectively. The in-vitro drug release results exhibited that the mSep@Chito NCs have a sustained release behavior with high pH-dependent properties. Cytotoxic results (MTT assay) showed that the sunitinib-loaded mSep@Chito2 NC had a significant cytotoxic effect on the MCF-7 cell lines. Also, the in-vitro compatibility of erythrocytes, physiological stability, biodegradability, and antibacterial and antioxidant activities of NCs was evaluated. The results showed that the synthesized NCs had excellent hemocompatibility, good antioxidant properties, and were sufficiently stable and biocompatible. Based on the antibacterial data, the minimal inhibitory concentration (MIC) values for mSep@Chito1, mSep@Chito2, and mSep@Chito3 were obtained as 125, 62.5, and 31.2 μg/mL towards S. aureus, respectively. All in all, the prepared NCs could be potentially used as a pH-triggered system for biomedical applications.

摘要

在这项研究中,通过共沉淀铁离子将磁铁矿纳米粒子固定在海泡石针上。然后,在柠檬酸(CA)的存在下,将得到的磁性海泡石(mSep)纳米颗粒用壳聚糖生物聚合物(Chito)包覆,以制备 mSep@Chito 核壳药物纳米载体(NCs)。TEM 图像显示,海泡石针上的磁性 FeO 纳米颗粒尺寸较小(小于 25nm)。对于 Chito 含量低和高的 NCs,阿昔替尼抗癌药物的载药效率分别为 ⁓45 和 83.7%。体外药物释放结果表明,mSep@Chito2 NC 具有持续释放行为,具有高 pH 依赖性。细胞毒性结果(MTT 测定)表明,载有阿昔替尼的 mSep@Chito2 NC 对 MCF-7 细胞系具有显著的细胞毒性作用。此外,还评估了 NCs 的体外红细胞相容性、生理稳定性、生物降解性、抗菌和抗氧化活性。结果表明,合成的 NCs 具有优异的血液相容性、良好的抗氧化性能,并且足够稳定和生物相容。根据抗菌数据,获得了 mSep@Chito1、mSep@Chito2 和 mSep@Chito3 对金黄色葡萄球菌的最小抑菌浓度(MIC)值分别为 125、62.5 和 31.2μg/mL。总之,所制备的 NCs 可潜在用作用于生物医学应用的 pH 触发系统。

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