N-Succinyl-chitosan systems for 5-aminosalicylic acid colon delivery: In vivo study with TNBS-induced colitis model in rats
N-Succinyl-chitosan systems for 5-aminosalicylic acid colon delivery: In vivo study with TNBS-induced colitis model in rats
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DOI：
10.1016/j.ijpharm.2011.06.025
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发表时间：
2011-09-15
影响因子：
5.8
通讯作者：
Diez-Sales, O.
中科院分区：
文献类型：
--
作者：
Mura, C.;Nacher, A.;Diez-Sales, O.
5-制备了氨基水杨酸（5-阿萨）N-琥珀酰壳聚糖（SucCH）微粒和冻干系统，作为潜在的结肠给药系统。先前评估了物理化学表征和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至结肠的良好候选物。在这项工作中，评估了这两种系统治疗炎症性肠道疾病的有效性。体外粘膜粘附研究表明，这两种系统对发炎的结肠粘膜具有优异的粘膜粘附特性。用2，4，6-三硝基苯磺酸（TNBS）直肠滴注雄性Wistar大鼠，诱发实验性结肠炎。以结肠/体重比、临床活动评分系统、髓过氧化物酶活性和组织学评价为炎症指标。将两种制剂与药物混悬液和SucCH混悬液进行比较。结果显示，将5-A5 A负载到SucCH聚合物中显著提高了大鼠诱导的结肠炎愈合的功效。(C)2011 Elsevier B. V.保留所有权利。
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-A5A into SucCH polymer markedly improved efficacy in the healing of induced colitis in rats. (C) 2011 Elsevier B.V. All rights reserved.