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Preparation and characterization of carboxymethyl cellulose containing quaternized chitosan for potential drug carrier

机译:含型药物载体含季壳聚糖羧甲基纤维素的制备与表征

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The objective of this study was to synthesize and characterize cystamine dihydrochloride (CYS) crosslinked carboxymethyl cellulose/quaternized chitosan (CMC/HACC) composite hydrogel film. Firstly, the glycidyl-based quaternary ammonium chitosan derivative (HACC) was synthesized using nucleophilic substitution reaction. Then HACC was analyzed by FTIR, (HNMR)-H-1 spectra and the composite films at different blending ratio of CMC and HACC were studied by rheology measurement, mechanical and swelling tests. When the composite films were prepared under optimized conditions (CMC: HACC = 7:1), they showed excellent mechanical properties (with improved 93.3% tensile strength and 2.3% elongation at break) and swellability (equilibrium swelling ratio increased 270%) compared to pure CMC film. 5-Fluorouracil (5-FU) was used as drug model which has broad-spectrum anticancer properties. The 5-FU/CMC/HACC composite films showed redox and pH responsive of drug release properties along with well biocompatibility. The in vitro cytotoxicity and cell apoptosis studies showed the drug loaded composite films with obvious toxicity against HepG2 cells especially in the presence of GSH. In addition, CMC/HACC composite films showed good antibacterial against S. aureus and E. coli, while pure CMC film had no antimicrobial activities. It can be concluded that CMC/HACC composite films can be potentially used as targeted drug delivery system. (C) 2019 Elsevier B.V. All rights reserved.
机译:本研究的目的是合成和表征半胱氨酸二盐酸盐(CYS)交联的羧甲基纤维素/季铵化壳聚糖(CMC / HACC)复合水凝胶膜。首先,使用亲核取代反应合成缩水甘油基季铵壳聚糖衍生物(HACC)。然后通过流变测量,机械和溶胀试验研究了通过FTIR,(HNMR)-H-1光谱和多种混合比的复合薄膜分析HACC。当在优化条件下制备复合膜(CMC:HACC = 7:1)时,它们显示出优异的机械性能(随着53.3%的拉伸强度和2.3%处于突破的伸长率),与溶胀性(平衡溶胀比增加270%)纯CMC薄膜。 5-氟尿嘧啶(5-FU)用作具有广谱抗癌性质的药物模型。 5-FU / CMC / HACC复合薄膜显示氧化还原和pH响应药物释放性能以及良好的生物相容性。体外细胞毒性和细胞凋亡研究表明,药物负载复合薄膜对HepG2细胞具有明显的毒性,特别是在GSH存在下。此外,CMC / HACC复合薄膜显示出对AUREUS和大肠杆菌的良好抗菌性,而纯CMC膜没有抗微生物活性。可以得出结论,CMC / HACC复合薄膜可以潜在地用作靶向药物递送系统。 (c)2019 Elsevier B.v.保留所有权利。

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