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New Grafted Copolymers Carrying Betaine Units Based on Gellan and N-Vinylimidazole as Precursors for Design of Drug Delivery Systems

机译:基于Gellan和N-乙烯基咪唑的新嫁接共聚物携带甜菜碱单位作为药物递送系统设计的前体

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摘要

New grafted copolymers possessing structural units of 1-vinyl-3-(1-carboxymethyl) imidazolium betaine were obtained by graft copolymerization of N-vinylimidazole onto gellan gum followed by the polymer-analogous reactions on grafted polymer with the highest grafting percentage using sodium chloroacetate as the betainization agent. The grafted copolymers were prepared using ammonium persulfate/N,N,N′,N′ tetramethylethylenediamine in a nitrogen atmosphere. The grafting reaction conditions were optimized by changing one of the following reaction parameters: initiator concentration, monomer concentration, polymer concentration, reaction time or temperature, while the other parameters remained constant. The highest grafting yield was obtained under the following reaction conditions: ci = 0.08 mol/L, cm = 0.8 mol/L, cp = 8 g/L, tr = 4 h and T = 50 °C. The kinetics of the graft copolymerization of N-vinylimidazole onto gellan was discussed and a suitable reaction mechanism was proposed. The evidence of the grafting reaction was confirmed through FTIR spectroscopy, X-ray diffraction, 1H-NMR spectroscopy and scanning electron microscopy. The grafted copolymer with betaine structure was obtained by a nucleophilic substitution reaction where the betainization agent was sodium chloroacetate. Preliminary results prove the ability of the grafted copolymers to bind amphoteric drugs (cefotaxime) and, therefore, the possibility of developing the new sustained drug release systems.
机译:具有1-乙烯基-3-(1-羧甲基)咪唑鎓甜菜碱的结构单元的新的接枝共聚物是通过将N-乙烯基咪唑接枝胶的共聚合,然后用氯乙酸钠接枝百分比的接枝聚合物上的聚合物 - 类似反应获得作为睡觉剂。在氮气氛中使用过硫酸铵/ N,N,N',N'四甲基乙基二氨基制备接枝的共聚物。通过改变以下反应参数之一优化接枝反应条件:引发剂浓度,单体浓度,聚合物浓度,反应时间或温度,而其他参数仍然是恒定的。在以下反应条件下获得最高的接枝产率:Ci = 0.08mol / L,Cm = 0.8mol / L,Cp = 8g / L,Tr = 4 h和T = 50℃。讨论了N-乙烯基咪唑接枝共聚的动力学,并提出了合适的反应机理。通过FTIR光谱,X射线衍射,1H-NMR光谱和扫描电子显微镜确认接枝反应的证据。通过亲核取代反应得到甜菜碱结构的接枝共聚物,其中壁型化剂是氯乙酸钠。初步结果证明了接枝的共聚物结合两性药物(头孢噻肟)的能力,以及因此开发新的持续药物释放系统的可能性。

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