Chitosan/Kollicoat SR 30D film-coated pellets of aminosalicylates for colonic drug delivery |
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| Authors: | He Wei Fan Li-Fang Bai Min Chang Yong-Zhen Xiang Bai Du Qing Wang Feng Qin Min Cao De-Ying |
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| Institution: | 1. Department of Pharmaceutics, School of Pharmaceutical Science, Hebei Medical University, ShiJiaZhuang, PR China;2. CSPC Pharmaceutical Technology Co., Ltd, ShiJiaZhuang, PR China;3. Department of Pharmaceutical Analysis, School of Pharmaceutical Science, Hebei Medical University, ShiJiaZhuang, PR China;4. Hebei Yiling Pharmaceutical Group, Medicine Institute, Beijing, PR China;5. XingTai Medical School Facial Feature & Medical Treatment Technic Faculty, Department of Pharmaceutics, XingTai Medical College, XingTai, PR China;6. Department of Hepatitis, National Institute for Communicable Disease Control and Prevention, Chinese Center for Disease Control and Prevention, Beijing, PR China;7. Department of Gastroenterology, Liuzhou Worker Hospital, Liuzhou, PR China |
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| 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 Cmax 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. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:186–195, 2010 |
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