PDF(Pubmed)
Abstract：
In this paper, a novel mono-methacrylated β-cyclodextrin (β-CD) monomer mediated by disulfide bond was synthesized, and then thermal copolymerized with HEMA monomer in the presence of a little crosslinker to prepare redox-responsive hydrogel for regulated drug delivery. The structure of the monomer was confirmed by FTIR, 1H NMR, 13C NMR spectroscopy. The substitution degree of polymerizable methacrylated group grafted onto β-CD was about 1 by calculating by1H NMR (0.987) and element analysis (0.937). The mono-methacrylated β-CD monomer can well copolymerize with 2-hydroxyethyl methacrylate (HEMA) monomer with gel fraction over 80%. The hydrogel shows low cytotoxicity, and copolymerization of the mono-methacrylated β-CD monomer in the hydrogels increases its equilibrium swelling degree (ESD) and tensile strength, while its transmittance slightly decreases. Drug loading and release rate are dependent on the β-CD content. The hydrogel with high β-CD content of 13.83 wt% shows 1.8 and 8.5 folds puerarin (PUE) and curcumin (CUR) loading than pure pHEMA hydrogel, respectively. The incorporation of β-CD sustained drug release, especially CUR release was prolonged more than 24 h from 5 h of pure pHEMA hydrogel (80% release). The hydrogels are highly sensitive to reduced glutathione (GSH), and low concentration of GSH of 3 mM can significantly accelerate drug release rate. The higher of β-CD content, the more sensitive the hydrogels to GSH, resulting in rapider drug release rate.
摘要：
在本文中,合成了一种由二硫键介导的单甲基丙烯酸酯化β-环糊精(β-CD)单体,然后在少量交联剂的存在下与HEMA单体热共聚以制备用于调节药物递送的氧化还原响应水凝胶。通过FTIR证实了单体的结构,1HNMR,13CNMR光谱。通过1HNMR（0.987）和元素分析（0.937）计算，接枝到β-CD上的可聚合甲基丙烯酸酯化基团的取代度为约1。单甲基丙烯酸酯化的β-CD单体可以与甲基丙烯酸2-羟乙酯（HEMA）单体很好地共聚，凝胶分数超过80％。水凝胶显示低细胞毒性，单甲基丙烯酸酯化β-CD单体在水凝胶中的共聚增加了其平衡溶胀度(ESD)和拉伸强度,而其透光率略有下降。药物负载和释放速率取决于β-CD含量。具有13.83wt％的高β-CD含量的水凝胶显示葛根素（PUE）和姜黄素（CUR）的负载是纯pHEMA水凝胶的1.8倍和8.5倍，分别。β-CD缓释药物的掺入，特别是CUR释放从5小时的纯pHEMA水凝胶（80％释放）延长超过24小时。水凝胶对还原型谷胱甘肽（GSH）高度敏感，3mM的低浓度GSH可以显着加速药物释放速率。β-CD含量越高,水凝胶对GSH越敏感，导致更快的药物释放速率。
