结肠药物靶向凝胶的体外降解及载药研究

In Vitro Biodegradability and Drug Release of Hydrogels for Colonic-site Drug Delivery

合成了丙烯酸丁酯,丙烯酸与二(甲基丙烯酰胺基)偶氮苯交联共聚的凝胶,主要研究了这类凝胶的pH敏感性、体外偶氮酶降解性及对模型药物(5-氨基水杨酸)的释放性能。在模拟的胃部环境中,凝胶几乎不溶胀,亦不降解,因而亦不释放药物;而在模拟的小肠环境中,凝胶释放药物的程度随平衡溶胀程度的增大而增大,通过调节凝胶的组成配比可以控制凝胶在小肠内的溶胀程度,进而避免凝胶内部的药物被提前释放。在含有偶氮酶缓冲溶液中凝胶释放药物的速率明显加快,释药程度显著提高,显示药物可完全释放在结肠内。

Biodegradable hydrogels based on butyl acrylate,acrylic acid cross-linked with 4,4′-di(methacryloylmino) azobenzene were prepared.Their pH-sensitivity and in vitro azo enzyme degradability as well as the release properties of 5-ASA as a model drug were researched.In the simulated stomach,the hydrogels hardly swelled and were not degraded,so the drugs inside them were not released.In the simulated intestine,the degree of drug release increased with the degree of equilibrium swelling,by adjusting the hydrogel...