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菊粉水凝胶作为结肠药物靶向载体:I. 甲基丙烯酸化菊粉的合成与表征及水凝胶的形成

Inulin hydrogels as carriers for colonic drug targeting: I. Synthesis and characterization of methacrylated inulin and hydrogel formation.

作者信息

Vervoort L, Van den Mooter G, Augustijns P, Busson R, Toppet S, Kinget R

机构信息

Laboratorium voor Farmacotechnologie en Biofarmacie, K.U. Leuven, Belgium.

出版信息

Pharm Res. 1997 Dec;14(12):1730-7. doi: 10.1023/a:1012179813102.

Abstract

PURPOSE

Vinyl groups were introduced in inulin chains in order to form hydrogels of this sugar polymer by free radical polymerization.

METHODS

Inulin was reacted with glycidyl methacrylate in N,N-dimethylformamide in the presence of 4-dimethylaminopyridine as catalyst. 1H and 13C NMR spectroscopy were used for the characterization of the obtained reaction product. Solid state 13C NMR spectroscopy revealed the conversion of the incorporated vinyl groups into covalent cross-links upon free radical polymerization of aqueous solutions of the derivatized inulin.

RESULTS

During reaction of inulin with glycidyl methacrylate, transesterification occurred, leading to the direct attachment of the methacryloyl group to inulin. Consequently, the obtained reaction product is methacrylated inulin. The extent of chemical modification of inulin could be tuned by varying the molar ratio of glycidyl methacrylate to inulin in the reaction mixture. Aqueous solutions of methacrylated inulin were converted into cross-linked hydrogels by free radical polymerization using ammonium persulphate and N,N,N',N'-tetramethylethylenediamine as initiating system.

CONCLUSIONS

Inulin hydrogels can be formed by free radical polymerization of aqueous solutions of methacrylated inulin.

摘要

目的

将乙烯基引入菊粉链中,以便通过自由基聚合形成这种糖聚合物的水凝胶。

方法

在4-二甲氨基吡啶作为催化剂的存在下,使菊粉与甲基丙烯酸缩水甘油酯在N,N-二甲基甲酰胺中反应。使用1H和13C核磁共振光谱对所得反应产物进行表征。固态13C核磁共振光谱显示,在衍生化菊粉水溶液的自由基聚合过程中,引入的乙烯基转化为共价交联键。

结果

在菊粉与甲基丙烯酸缩水甘油酯反应过程中发生了酯交换反应,导致甲基丙烯酰基直接连接到菊粉上。因此,所得反应产物是甲基丙烯酰化菊粉。通过改变反应混合物中甲基丙烯酸缩水甘油酯与菊粉的摩尔比,可以调节菊粉的化学改性程度。使用过硫酸铵和N,N,N',N'-四甲基乙二胺作为引发体系,通过自由基聚合将甲基丙烯酰化菊粉的水溶液转化为交联水凝胶。

结论

通过甲基丙烯酰化菊粉水溶液的自由基聚合可以形成菊粉水凝胶。

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