N-Succinyl-chitosan systems for 5-aminosalicylic acid colon delivery: In vivo study with TNBS-induced colitis model in rats

被引：77

作者：

Mura, C. ^{[1
,2
]}

Nacher, A. ^{[1
,3
]}

Merino, V. ^{[1
,3
]}

Merino-Sanjuan, M. ^{[1
,3
]}

Carda, C. ^{[4
]}

Ruiz, A. ^{[4
]}

Manconi, M. ^{[2
]}

Loy, G. ^{[2
]}

Fadda, A. M. ^{[2
]}

Diez-Sales, O. ^{[1
,3
]}

机构：

[1] Univ Valencia, Fac Pharm, Dept Pharm & Pharmaceut Technol, E-46100 Burjassot, Valencia, Spain

[2] Univ Cagliari, Dept Farmaco Chim Tecnol, I-09124 Cagliari, Italy

[3] Univ Valencia, Univ Politecn Valencia, Ctr Mixto, Inst Reconocimiento Mol & Desarrollo Tecnol, E-46100 Burjassot, Valencia, Spain

[4] Univ Valencia, Fac Med & Dent, Dept Pathol, E-46100 Burjassot, Valencia, Spain

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2011年 / 416卷 / 01期

关键词：

N-Succinyl-chitosan systems; 5-Aminosalicylic acid; Colon delivery; TNBS induced colitis; INFLAMMATORY-BOWEL-DISEASE; TARGETED DRUG-DELIVERY; ULCERATIVE-COLITIS; CAPSULES; DESIGN; MUCOSA; VITRO; MICE;

D O I：

10.1016/j.ijpharm.2011.06.025

中图分类号：

R9 [药学];

学科分类号：

100702 [药剂学];

摘要：

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.

引用

页码：145 / 154

页数：10

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