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将 GMA 和一些共聚单体接枝到壳聚糖上,用于控制释放双氯芬酸钠。

Grafting of GMA and some comonomers onto chitosan for controlled release of diclofenac sodium.

机构信息

Department of Chemistry, DAV College, Jalandhar, Punjab 144008, India.

Punjab Technical University, Jalandhar-Kapurthala Highway, Kapurthala, Punjab 144601, India.

出版信息

Int J Biol Macromol. 2014 Mar;64:368-76. doi: 10.1016/j.ijbiomac.2013.12.028. Epub 2013 Dec 24.

Abstract

In order to develop pH sensitive hydrogels for controlled drug release we have graft copolymerized glycidyl methacrylate (GMA) with comonomers acrylic acid, acrylamide and acrylonitrile, onto chitosan (Ch) by using potassium persulphate (KPS) as free radical initiator in aqueous solution. The optimum percent grafting for GMA was recorded for 1g chitosan at [KPS]=25.00 × 10(-3)mol/L, [GMA]=0.756 × 10(-3)mol/L, reaction temperature=60 °C and reaction time=1h in 20 mL H2O. Binary monomers were grafted for five different concentrations at optimum grafting conditions evaluated for GMA alone onto chitosan. The graft copolymers were characterized by FTIR, XRD, TGA and SEM. The swelling properties of chitosan and graft copolymers were investigated at different pH to define their end uses in sustained release of an anti-inflammatory drug, diclofenac sodium. Percent drug release w.r.t. drug loaded in polymeric sample was studied as function of time in buffer solutions of pH 2.0 and 7.4. In vitro release data was analyzed using Fick's Law. Chitosan grafted with binary monomers, GMA-co-AAm and GMA-co-AN showed very good results for sustained release of drug at 7.4 pH.

摘要

为了开发用于控制药物释放的 pH 敏感水凝胶,我们使用过硫酸钾 (KPS) 作为自由基引发剂,在水溶液中将甲基丙烯酸缩水甘油酯 (GMA) 与共聚单体丙烯酸、丙烯酰胺和丙烯腈接枝到壳聚糖 (Ch) 上。对于 1g 壳聚糖,在 [KPS]=25.00×10(-3)mol/L、[GMA]=0.756×10(-3)mol/L、反应温度=60°C 和反应时间=1h 的最佳接枝条件下,GMA 的最佳接枝率为 20 mL H2O。在单独评估 GMA 接枝到壳聚糖的最佳接枝条件下,用五种不同浓度的二元单体接枝。通过 FTIR、XRD、TGA 和 SEM 对接枝共聚物进行了表征。在不同 pH 值下研究了壳聚糖和接枝共聚物的溶胀性能,以确定它们在抗炎药物双氯芬酸钠的缓释中的最终用途。研究了在 pH 值为 2.0 和 7.4 的缓冲溶液中,药物在聚合物样品中的负载量与药物释放百分比随时间的关系。使用菲克定律分析体外释放数据。在 7.4 pH 下,接枝有二元单体 GMA-co-AAm 和 GMA-co-AN 的壳聚糖在药物缓释方面表现出非常好的效果。

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