Dept. Farmaco Chimico Tecnologico, University of Cagliari, Cagliari 09124, Italy.
Int J Pharm. 2011 Sep 15;416(1):145-54. doi: 10.1016/j.ijpharm.2011.06.025. Epub 2011 Jun 23.
5-Aminosalicylic acid (5-ASA) loaded N-Succinyl-chitosan (SucCH) microparticle and freeze-dried system were prepared as potential delivery systems to the colon. Physicochemical characterization and in vitro release and swelling studies were previously assessed and showed that the two formulations appeared to be good candidates to deliver the drug to the colon. In this work the effectiveness of these two systems in the treatment of inflammatory bowel disease was evaluated. In vitro mucoadhesive studies showed excellent mucoadhesive properties of both the systems to the inflamed colonic mucosa. Experimental colitis was induced by rectal instillation of 2,4,6-trinitrobenzene sulfonic acid (TNBS) into male Wistar rats. Colon/body weight ratio, clinical activity score system, myeloperoxidase activity and histological evaluation were determined as inflammatory indices. The two formulations were compared with drug suspension and SucCH suspension. The results showed that the loading of 5-ASA into SucCH polymer markedly improved efficacy in the healing of induced colitis in rats.
5-氨基水杨酸（5-ASA）负载 N-琥珀酰壳聚糖（SucCH）微球和冷冻干燥系统被制备为潜在的结肠递药系统。先前已经评估了其理化性质、体外释放和溶胀研究，结果表明这两种制剂似乎是将药物递送到结肠的良好候选物。在这项工作中，评估了这两种系统在治疗炎症性肠病中的有效性。体外黏膜黏附研究表明，两种系统对发炎的结肠黏膜均具有极好的黏膜黏附特性。通过直肠内注入 2,4,6-三硝基苯磺酸（TNBS）诱导雄性 Wistar 大鼠实验性结肠炎。将结肠/体重比、临床活动评分系统、髓过氧化物酶活性和组织学评估作为炎症指标进行测定。将这两种制剂与药物混悬液和 SucCH 混悬液进行了比较。结果表明，将 5-ASA 载入 SucCH 聚合物可显著提高治疗大鼠诱导性结肠炎的疗效。
