title: Investigation of the colon-targeting, improvement on the side-effects and therapy on the experimental colitis in mouse of a resin microcapsule loading dexamethasone sodium phosphate.
abstract: BACKGROUND
  Dexamethasone is the major drug in the treatment of ulcerative colitis (UC). However, the extensive or long-time use of dexamethasone causes many toxic side-effects. Ion exchange resins react with external-ions through their own functional groups and Eudragit S occurs degradation when pH > 7. These features make them suitable for oral delivery system.
  
  
  OBJECTIVE
  Resin microcapsule (DRM) composed by 717 anion exchange resin and Eudragit S100 was used to target dexamethasone to the colon to improve its treatment effect on UC and reduce its toxic side-effects.
  
  
  RESULTS
  Dexamethasone sodium phosphate (DXSP) was sequentially encapsulated in 717 anion-exchange resin and Eudragit S100 to prepare the DXSP-loaded resin microcapsule (DXSP-DRM). The in vitro release study and in vivo study of pharmacokinetics and the intestinal drug residues in rat demonstrated the good colon-targeting of DXSP-DRM. Moreover, the DXSP-DRM can reduce the toxic side-effects induced by DXSP and have good therapeutic effects on colitis mouse induced by 2,4,6-trinitrobenzenesulfonic acid.
  
  
  CONCLUSIONS
  Dexamethasone can be targeted to the colon by DRM, thereby enhancing its treatment effect and reducing its toxic side effects.
  
  
  CONCLUSIONS
  The resin microcapsule system has good colon-targeting and can be used in the development of colon-targeted preparations.
authors.affiliation: a School of Pharmacy, Xi'an Jiaotong University , Xi'an , Shaanxi , China .
authors.forename: Aiguo
authors.initials: A
authors.lastname: Zeng
authors.affiliation: a School of Pharmacy, Xi'an Jiaotong University , Xi'an , Shaanxi , China .
authors.forename: Kai
authors.initials: K
authors.lastname: Dong
authors.affiliation: b Qilu Hospital of Shandong University , Qingdao , Shandong , China , and.
authors.forename: Maoling
authors.initials: M
authors.lastname: Wang
authors.affiliation: c Department of Pharmacy , the First Affiliated Hospital of Medical College, Xi'an Jiaotong University , Xi'an , Shaanxi , China.
authors.forename: Jinyao
authors.initials: J
authors.lastname: Sun
authors.affiliation: c Department of Pharmacy , the First Affiliated Hospital of Medical College, Xi'an Jiaotong University , Xi'an , Shaanxi , China.
authors.forename: Yalin
authors.initials: Y
authors.lastname: Dong
authors.affiliation: a School of Pharmacy, Xi'an Jiaotong University , Xi'an , Shaanxi , China .
authors.forename: Ke
authors.initials: K
authors.lastname: Wang
authors.affiliation: a School of Pharmacy, Xi'an Jiaotong University , Xi'an , Shaanxi , China .
authors.forename: Chenning
authors.initials: C
authors.lastname: Guo
authors.affiliation: a School of Pharmacy, Xi'an Jiaotong University , Xi'an , Shaanxi , China .
authors.forename: Yan
authors.initials: Y
authors.lastname: Yan
authors.affiliation: a School of Pharmacy, Xi'an Jiaotong University , Xi'an , Shaanxi , China .
authors.forename: Lu
authors.initials: L
authors.lastname: Zhang
authors.affiliation: a School of Pharmacy, Xi'an Jiaotong University , Xi'an , Shaanxi , China .
authors.forename: Xianpeng
authors.initials: X
authors.lastname: Shi
authors.affiliation: a School of Pharmacy, Xi'an Jiaotong University , Xi'an , Shaanxi , China .
authors.forename: Jianfeng
authors.initials: J
authors.lastname: Xing
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D000837:Anion Exchange Resins / Q000737:chemistry* / Q000493:pharmacokinetics; D002214:Capsules / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics*; D003092:Colitis / Q000188:drug therapy*; D003106:Colon / Q000737:chemistry / Q000378:metabolism*; D003907:Dexamethasone / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D006863:Hydrogen-Ion Concentration; D051379:Mice; D051381:Rats; D014302:Trinitrobenzenesulfonic Acid / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000180:Acrylic Resins; D000837:Anion Exchange Resins; D002214:Capsules; C004180:dexamethasone 21-phosphate; D003907:Dexamethasone; D014302:Trinitrobenzenesulfonic Acid
keywords: Anion exchage resin; colon-targeting; dexamethasone sodium phosphate; side-effects; ulcerative colitis