Basic Research
Copyright ©2005 Baishideng Publishing Group Inc. All rights reserved.
World J Gastroenterol. Dec 21, 2005; 11(47): 7457-7460
Published online Dec 21, 2005. doi: 10.3748/wjg.v11.i47.7457
Colon-specific drug delivery systems based on cyclodextrin prodrugs: In vivo evaluation of 5-aminosalicylic acid from its cyclodextrin conjugates
Mei-Juan Zou, Gang Cheng, Hirokazu Okamoto, Xiu-Hua Hao, Feng An, Fu-De Cui, Kazumi Danjo
Mei-Juan Zou, Gang Cheng, Xiu-Hua Hao, Feng An, Fu-De Cui, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, Liaoning Province, China
Hirokazu Okamoto, Kazumi Danjo, Faculty of Pharmacy, Meijo University, 150 Yagotoyama, Tempaku-ku, Nagoya 468-8503, Japan
Author contributions: All authors contributed equally to the work.
Correspondence to: Gang Cheng, School of Pharmacy, Shenyang Pharmaceutical University, PO Box 32, 103 Wenhua Road, Shenhe District, Shenyang 110016, Liaoning Province, China. chenggang1963@hotmail.com
Telephone: +86-24-23986326 Fax: +86-24-23903547
Received: May 25, 2004
Revised: August 13, 2005
Accepted: August 17, 2005
Published online: December 21, 2005
Abstract

AIM: To investigate the release of cyclodextrin-5-aminosalicylic acid (CyD-5-ASA) in cecum and colon.

METHODS: An anti-inflammatory drug 5-ASA was conjugated onto the hydroxyl groups of α-, β- and γ-cyclodextrins (CyDs) through an ester linkage, and the in vivo drug release behavior of these prodrugs in rat’s gastrointestinal tract after the oral administration was investigated.

RESULTS: The 5-ASA concentration in the rat’s stomach and small intestine after the oral administration of CyD-5-ASA conjugate was much lower than that after the oral administration of 5-ASA alone. The lower concentration was attributable to the passage of the conjugate through the stomach and small intestine without significant degradation or absorption, followed by the degradation of the conjugate site-specific in the cecum and colon. The oral administration of CyD-5-ASA resulted in lower plasma and urine concentration of 5-ASA than that of 5-ASA alone.

CONCLUSION: CyD-5-ASA conjugates may be used as prodrugs for colon-specific drug delivery system.

Keywords: Cyclodextrin; 5-Aminosalicylic acid; In vivo; Colon-specific