N, N, N-三甲基壳聚糖纳米微球的合成及其对姜黄素缓释的影响

IF 4.6 Q1 CHEMISTRY, APPLIED
Xueqin Zhao , Chao Lu , Songlin Yang , Rui Ni , Tianqing Peng , Jin Zhang
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引用次数: 2

摘要

为了提高姜黄素的生物利用度,克服组织屏障,如血脑屏障,开发一种表面带正电荷的亲水性药物载体至关重要。本文制备了一种季铵化壳聚糖衍生物N,N,N-三甲基壳聚糖(TMC),它是一种阳离子多糖。利用核磁共振(1H-NMR)和红外光谱(FTIR)对TMC的合成进行了验证。研究了一种简单的纳米乳法制备负载姜黄素的纳米球。可观察到高封装效率(90%以上)。2.5 mg/mL和4.0 mg/mL的TMC制备的纳米球的平均粒径分别为555.3±117.7 nm和771.2±123.2 nm。研究了TMC浓度对其释放曲线的影响。结果表明,当TMC的浓度达到4.0 mg/mL时,姜黄素的释放时间延长,且随着释放时间的增加,姜黄素的释放动力学呈一级释放,且其释放动力学也受pH值的影响。此外,细胞毒性研究表明,用合成TMC处理细胞时,没有发现毒性作用。姜黄素负载TMC纳米球处理的小鼠心脏内皮细胞的相对细胞活力高于单独姜黄素处理的细胞。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis of N, N, N-trimethyl chitosan-based nanospheres for the prolonged release of curcumin

It is critical to develop a hydrophilic drug carrier with positive charge on the surface to enhance the bioavailability of curcumin to overcome the tissue barrier, e.g., blood brain barrier. In this paper, a quaternized chitosan derivative, N,N,N-Trimethyl Chitosan (TMC) was produced which is a cationic polysaccharide. Nuclear magnetic resonance (1H-NMR) and Infrared Spectroscopy (FTIR) have been used to verify the synthesis of TMC. A simple nanoemulsion process has been developed to produce TMC-based nanosphere to load curcumin. A high encapsulation efficiency (over 90%) can be observed. The average particle size of nanospheres made of TMC with 2.5 mg/mL and 4.0 mg/ mL is estimated at 555.3±117.7 nm and 771.2±123.2 nm, respectively. The effect of the concentrations of TMC on the release profile has been investigated. It is found that nanospheres made of a higher concentration of TMC, 4.0 mg/mL, could lead to an extended release of curcumin, and the first-order release kinetics can be observed when release time increases from 0 to 265 h. The release kinetics of curcumin loaded in TMC nanospheres is also influenced by pH value. In addition, the cytotoxicity study shows that no toxic effect can be found when cells are treated with synthetic TMC. The relative cell viability of mouse cardiac endothelial cells treated with curcumin loaded TMC nanospheres is higher than that when cells treated with curcumin alone.

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来源期刊
CiteScore
4.50
自引率
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审稿时长
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