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基于聚乙二醇-羧甲基壳聚糖的 pH 响应水凝胶:光诱导合成、表征、溶胀及作为潜在药物载体的体外评价。

Poly(ethylene glycol)-carboxymethyl chitosan-based pH-responsive hydrogels: photo-induced synthesis, characterization, swelling, and in vitro evaluation as potential drug carriers.

机构信息

Polymer Laboratory, Chemistry Department, Faculty of Science, Mansoura University, ET-35516 Mansoura, Egypt.

出版信息

Carbohydr Res. 2010 Sep 23;345(14):2004-12. doi: 10.1016/j.carres.2010.07.026. Epub 2010 Jul 21.

Abstract

In this study, carboxymethyl chitosan was prepared, characterized, and then photo-induced graft copolymerized with poly(ethylene glycol) under a nitrogen atmosphere in aqueous solution using 2,2-dimethoxy-2-phenyl acetophenone (DMPA) as the photo-initiator. The grafting copolymerization process was confirmed and the resulting copolymers were characterized using differential scanning calorimetry (DSC), FTIR spectroscopy, 2D-X ray diffraction, and elemental analysis. The kinetics of the grafting reactions was also studied. Under the applied experimental conditions, the optimum grafting values were obtained at: CMCs=0.2 g, PEGA=249 mM, DMPA=10.4 mM at a 2 h reaction time. Some of the resulting copolymers were selected and used in the presence of methylene bisacrylamide (MBA) as a crosslinking agent to develop pH-responsive hydrogel matrices. The swelling characteristics and the in vitro release profiles of 5-fluorouracil (5-FU), as a model drug, from the hydrogels were investigated. The results revealed that the hydrogel matrices developed in this study can be customized to act as good candidates in drug delivery systems.

摘要

在这项研究中,羧甲基壳聚糖被制备、表征,并在氮气气氛下,在水溶液中使用 2,2-二甲氧基-2-苯基苯乙酮 (DMPA) 作为光引发剂,光诱导接枝共聚聚乙二醇。接枝共聚过程得到了确认,并使用差示扫描量热法(DSC)、傅里叶变换红外光谱(FTIR)、二维 X 射线衍射和元素分析对所得共聚物进行了表征。还研究了接枝反应的动力学。在应用的实验条件下,在 CMCs=0.2 g、PEGA=249 mM、DMPA=10.4 mM 的条件下,反应时间为 2 小时,可获得最佳接枝值。选择部分所得共聚物,并在亚甲基双丙烯酰胺 (MBA) 的存在下用作交联剂,以开发对 pH 有响应的水凝胶基质。研究了水凝胶对 5-氟尿嘧啶 (5-FU) 作为模型药物的溶胀特性和体外释放曲线。结果表明,本研究中开发的水凝胶基质可以定制为药物传递系统的良好候选物。

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