title: Colon-specific drug delivery systems based on cyclodextrin prodrugs: in vivo evaluation of 5-aminosalicylic acid from its cyclodextrin conjugates.
abstract: OBJECTIVE
  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 alpha-, beta- and gamma-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.
  
  
  CONCLUSIONS
  CyD-5-ASA conjugates may be used as prodrugs for colon-specific drug delivery system.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenhe District, Shenyang 110016, Liaoning Province, China.
authors.forename: Mei-Juan
authors.initials: MJ
authors.lastname: Zou
authors.forename: Gang
authors.initials: G
authors.lastname: Cheng
authors.forename: Hirokazu
authors.initials: H
authors.lastname: Okamoto
authors.forename: Xiu-Hua
authors.initials: XH
authors.lastname: Hao
authors.forename: Feng
authors.initials: F
authors.lastname: An
authors.forename: Fu-De
authors.initials: FD
authors.lastname: Cui
authors.forename: Kazumi
authors.initials: K
authors.lastname: Danjo
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics*; D003106:Colon; D003505:Cyclodextrins / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems / Q000379:methods*; D007408:Intestinal Absorption; D008297:Male; D019804:Mesalamine / Q000493:pharmacokinetics*; D011355:Prodrugs / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D003505:Cyclodextrins; D011355:Prodrugs; D019804:Mesalamine