title: Chitosan/Kollicoat SR 30D film-coated pellets of aminosalicylates for colonic drug delivery.
abstract: The purpose of the study was to (i) prepare the chitosan/Kollicoat SR 30D film-coated pellets for colonic drug delivery, and (ii) evaluate the colonic delivery and efficacy of these coated pellets in the rat. The pellets were coated to different film thickness with chitosan/Kollicoat SR 30D formulations. In vitro drug release was assessed in simulated gastrointestinal (GI) tract conditions. Biodistribution of aminosalicylates (5-ASA) in GI tract and plasma was measured after oral administration of coated or uncoated 5-ASA pellets. Efficacy of the coated or uncoated 5-ASA pellets was tested in 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced rat colitis model. Healing of induced colitis was assessed by measuring the myeloperoxidase activities, colon wet weight/body weight, and damage score. The coating was susceptible to bacteria digestion, resulting in an increase in the release of 5-ASA from the coated pellets. After administration of the coated pellets, the drug concentration in the large intestine was higher than those of uncoated pellets. In plasma, the observed mean C(max) from the coated pellets was significantly lower than that of the uncoated pellets. Chitosan/Kollicoat SR 30D film-coated pellets could deliver the 5-ASA to the targeted site, providing effective treatment for inflammatory bowel disease.
authors: Department of Pharmaceutics, School of Pharmaceutical Science, Hebei Medical University, ShiJiaZhuang, PR China. hhewwei@126.com
authors: He
authors: H
authors: Wei
authors: Fan
authors: F
authors: Li-Fang
authors: Bai
authors: B
authors: Min
authors: Chang
authors: C
authors: Yong-Zhen
authors: Xiang
authors: X
authors: Bai
authors: Du
authors: D
authors: Qing
authors: Wang
authors: W
authors: Feng
authors: Qin
authors: Q
authors: Min
authors: Cao
authors: C
authors: De-Ying
mesh_terms: D000636:Aminosalicylic Acids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D048271:Chitosan / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D003106:Colon / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D015212:Inflammatory Bowel Diseases / Q000188:drug therapy; D008297:Male; D008855:Microscopy, Electron, Scanning; D011145:Polyvinyls / Q000737:chemistry*; D051381:Rats; D012995:Solubility; D013499:Surface Properties; D013608:Tablets, Enteric-Coated; D014018:Tissue Distribution
chemical_list: D000636:Aminosalicylic Acids; D004337:Drug Carriers; D011145:Polyvinyls; D013608:Tablets, Enteric-Coated; C013215:polyvinyl acetate; D048271:Chitosan