中国光学, 2018, 11 (3): 420, 网络出版: 2018-07-24   

壳聚糖基聚合物碳点荧光材料合成及其自组装载药应用

Synthesis of chitosan-based polymer carbon dots fluorescent materials and application of self-assembled drug-loading
作者单位
广西师范学院 化学与材料科学学院, 广西 南宁530001
摘要
荧光碳点具有化学稳定性好、毒性小、可表面功能化等优点, 引起了人们极大的兴趣。近年来, 由高分子多糖合成的聚合物碳点成为另一研究热点。本文通过水热法合成了一种壳聚糖基荧光聚合物碳点材料(P(CS-g-mPEG-CA)CDs), 并用于载药研究。基于壳聚糖和聚乙二醇既是碳点的碳源也是碳点的钝化试剂, 本文选择壳聚糖接枝聚乙二醇单甲醚和柠檬酸衍生物作为聚合物碳点的碳源, 以提高聚合碳点的量子产率。另外, 聚合物碳点还可以保留聚乙二醇与壳聚糖分子结构, 为其在载药方面的应用提供有利条件。采用红外光谱、紫外光谱、X射线衍射、光电子能谱、透射电子显微镜和光致发光光谱对P(CS-g-mPEG-CA)CDs进行了结构表征以及pH值稳定性的测试。结果表明, 所合成的P(CS-g-mPEG-CA)CDs具有较高的荧光量子产率(6681%)、较长的荧光寿命(15247 ns)、良好的pH稳定性。以阿霉素为模型药物, 利用该聚合物碳点进行了负载研究, 结果表明, 当聚乙二醇单甲醚取代度为119%时, 聚合物碳点的载药量最高为513%, 最大药物释放率为287%, 此外, 药物的装载和释放可以通过mPEG的接枝率进行控制。采用MTT法评价了聚合物的碳点对鼻咽癌细胞(CNE-2)的毒性作用。研究表明, 空白聚合物碳点无明显细胞毒性, CNE-2细胞存活率随着载药胶束的增加而降低, 说明载药胶束对CNE-2细胞有较强的抑制作用。可见该P(CS-g-mPEG-CA)CDs在荧光标记、药物递送、荧光示踪系统和控制释放方面, 具有一定的应用前景。
Abstract
Fluorescent carbon dots have the advantages of good chemical stability, low toxicity, and surface functionalization, which has caused concern. In recent years, polymer carbon dots synthesize by polymer polysaccharides have become a new research hotspot. In this paper, a chitosan-based fluorescent polymer carbon dot material is synthesized by hydrothermal method and used for drug-loading research. We choose chitosan-graft-polyethylene glycol monomethyl ether and citric acid derivatives as the carbon sources for the carbon dots, because chitosan and polyethylene glycol are both a carbon source for carbon dots and a passivation reagent for carbon dots. Then the quantum yield of the polymeric carbon dots is increased. Polymer carbon dots can also retain the molecular structure of polyethylene glycol and chitosan, providing favorable conditions for its application in drug loading. The structural characterization is performed on P(CS-g-mPEG-CA)CDs by IR, UV, X-ray diffraction, photoelectron spectroscopy, transmission electron microscopy and photoluminescence spectra and pH stability test is carried out. The results show that the synthesized P(CS-g-mPEG-CA)CDs has higher fluorescence quantum yield(6681%), longer fluorescence lifetime(15247 ns), and better pH stability. Using Doxorubicin as a model drug, a load study was conducted using this polymer carbon dot. The results show that if the degree of substitution of mPEG is 119%, the maximum loading rate of polymer carbon dots is 513% and the maximum drug release rate is 287%. In addition, we also found that drug loading and release could be controlled by the grafting rate of mPEG. In addition, the cytotoxicity of polymer carbon dots on nasopharyngeal carcinoma cells(CNE-2) is evaluated using an MTT assay. The study shows that there is no obvious cytotoxicity of blank P(CS-g-mPEG-CA)CDs, and that the survival rate of CNE-2 cells decreases with the increase of drug-loaded micelles. The results show that the P(CS-g-mPEG-CA)CDs have a certain application prospect in the aspects of fluorescence labeling, drug delivery, fluorescent tracer system and controlled release.

于淑娟, 陈宽, 汪丰, 朱永飞. 壳聚糖基聚合物碳点荧光材料合成及其自组装载药应用[J]. 中国光学, 2018, 11(3): 420. YU Shu-juan, CHEN Kuan, WANG Feng, ZHU Yong-fei. Synthesis of chitosan-based polymer carbon dots fluorescent materials and application of self-assembled drug-loading[J]. Chinese Optics, 2018, 11(3): 420.

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