Synthesis and properties of degradable hydrogels of konjac glucomannan grafted acrylic acid for colon-specific drug delivery

Synthesis and properties of degradable hydrogels of konjac glucomannan grafted acrylic acid for colon-specific drug delivery
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DOI:
10.1016/j.polymer.2005.05.041
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发表时间:
2005-07-25
期刊:
影响因子:
4.6
通讯作者:
Zhuo, RX
Zhuo, RX
中科院分区:
化学2区
文献类型:
--
作者:
Chen, LG;Liu, ZL;Zhuo, RX

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本文报道了一种新型结肠靶向给药水凝胶系统的合成和性质。该凝胶由葡甘聚糖(KGM)与丙烯酸(AA)共聚,N,N-亚甲基双丙烯酰胺(MBAAm)交联而成。研究了各种参数对水凝胶平衡溶胀率的影响。溶胀率与MBAAm含量成反比。可以通过改变聚合物的交联密度来调节凝胶的溶胀程度。凝胶的溶胀率对环境pH值的变化有敏感的响应。降解实验结果表明,该水凝胶保持了魔芋葡甘聚糖的酶降解特性,在纤维素酶E0240作用下,5天降解率可达52.5%。本文研究了模型药物5-氨基水杨酸(5-ASA)在纤维素酶E0240存在下,在pH7.4的磷酸盐缓冲液中于37 ℃的体外释放。36h后5-ASA的累积释放率达95.19%,药物释放受凝胶溶胀和降解的控制。(c)2005 Elsevier Ltd.保留所有权利。
In this paper, we reported the synthesis and properties of novel hydrogel systems designed for colon targeted drug delivery. The gels were composed of konjac glucomannan (KGM), copolymerized with acrylic acid (AA) and cross-linked by N,N-methylene-bis-(acrylamide) (MBAAm). The influence of various parameters on the equilibrium swelling ratios of the hydrogels was investigated. The swelling ratio was inversely proportional to the content of MBAAm. It was possible to modulate the degree of swelling of the gels by changing cross-linking density of the polymer. The gels' swelling ratio has sensitive respondence to the environmental pH value variation. The results of degradation test show that the hydrogels retain the enzymatic degradation character of KGM and they can be degraded for 52.5% in 5 days by Cellulase E0240. In vitro release of model drug 5-aminosalicylic acid (5-ASA) was studied in the presence of Cellulase E0240 in pH 7.4 phosphate buffer at 37 C. The accumulative release percent of 5-ASA reached 95.19% after 36 h and the drug release was controlled by the swelling and degradation of the hydrogels. (c) 2005 Elsevier Ltd. All rights reserved.