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

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 ap...

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Bibliographic Details
Published in:International journal of pharmaceutics 2011-09, Vol.416 (1), p.145-154
Main Authors: Mura, C., Nácher, A., Merino, V., Merino-Sanjuan, M., Carda, C., Ruiz, A., Manconi, M., Loy, G., Fadda, A.M., Diez-Sales, O.
Format: Article
Language:English
Subjects:
5-Aminosalicylic acid
Absorption
Animals
Anti-Inflammatory Agents, Non-Steroidal - administration & dosage
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics
Anti-Inflammatory Agents, Non-Steroidal - therapeutic use
Biological and medical sciences
body weight
Chitosan - chemistry
colitis
Colitis - chemically induced
Colitis - drug therapy
Colitis - metabolism
Colitis - pathology
colon
Colon - drug effects
Colon - metabolism
Colon - pathology
Colon delivery, TNBS induced colitis
Disease Models, Animal
Drug Carriers - administration & dosage
Drug Carriers - chemistry
Drug Carriers - metabolism
Drug Carriers - pharmacokinetics
Drug Carriers - therapeutic use
Drug Delivery Systems - methods
drugs
freeze drying
Freeze Drying - methods
General pharmacology
in vivo studies
Intestinal Mucosa - drug effects
Intestinal Mucosa - pathology
Lymphocyte Activation - drug effects
Male
Medical sciences
Mesalamine - administration & dosage
Mesalamine - chemistry
Mesalamine - pharmacokinetics
Mesalamine - therapeutic use
mucosa
myeloperoxidase
N-Succinyl-chitosan systems
Organ Size - drug effects
Peroxidase - metabolism
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
polymers
Polymers - chemical synthesis
Polymers - chemistry
Polymers - metabolism
Polymers - pharmacokinetics
Polymers - therapeutic use
Rats
Rats, Wistar
sulfonic acid
Trinitrobenzenesulfonic Acid
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Summary: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.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2011.06.025