title: Mucoadhesive microparticulates based on polysaccharide for target dual drug delivery of 5-aminosalicylic acid and curcumin to inflamed colon.
abstract: In this work, thiolated chitosan/alginate composite microparticulates (CMPs) coated by Eudragit S-100 were developed for colon-specific delivery of 5-aminosalicylic acid (5-ASA) and curcumin (CUR), and the use of it as a multi drug delivery system for the treatment of colitis. The physicochemical properties of the CMPs were evaluated. In vitro release was performed in gradually pH-changing medium simulating the conditions of different parts of GIT, and the results showed that the Eudragit S-100 coating has a pH-sensitive release property, which can avoid drug being released at a pH lower than 7. An everted sac method was used to evaluate the mucoadhesion of CMPs. Ex vivo mucoadhesive tests showed CMPs have excellent mucosa adhesion for the colonic mucosa of rats. In vivo treatment effect of enteric microparticulates systems was evaluated in colitis rats. The results showed superior therapeutic efficiency of this drug delivery system for the colitis rats induced by TNBS. Therefore, the enteric microparticulates systems combined the properties of pH dependent delivery, mucoadhesive, and control release, and could be an available tool for the treatment of human inflammatory bowel disease.
authors.affiliation: Department of Chemistry, Lanzhou University, Lanzhou 730000, PR China; Department of Pharmacy, The First Hospital of Lanzhou University, Lanzhou 730000, PR China.
authors.forename: Haogang
authors.initials: H
authors.lastname: Duan
authors.affiliation: Department of Chemistry, Lanzhou University, Lanzhou 730000, PR China.
authors.forename: Shaoyu
authors.initials: S
authors.lastname: Lü
authors.affiliation: Department of Chemistry, Lanzhou University, Lanzhou 730000, PR China.
authors.forename: Chunmei
authors.initials: C
authors.lastname: Gao
authors.affiliation: Department of Chemistry, Lanzhou University, Lanzhou 730000, PR China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Bai
authors.affiliation: Department of Pharmacy, The First Hospital of Lanzhou University, Lanzhou 730000, PR China.
authors.forename: Hongyan
authors.initials: H
authors.lastname: Qin
authors.affiliation: Department of Pharmacy, The First Hospital of Lanzhou University, Lanzhou 730000, PR China.
authors.forename: Yuhui
authors.initials: Y
authors.lastname: Wei
authors.affiliation: Department of Pharmacy, The First Hospital of Lanzhou University, Lanzhou 730000, PR China.
authors.forename: Xin'an
authors.initials: X
authors.lastname: Wu
authors.affiliation: Department of Chemistry, Lanzhou University, Lanzhou 730000, PR China. Electronic address: mzliu@lzu.edu.cn.
authors.forename: Mingzhu
authors.initials: M
authors.lastname: Liu
mesh_terms: D000818:Animals; D048271:Chitosan / Q000737:chemistry; D003092:Colitis / Q000188:drug therapy; D003106:Colon / Q000276:immunology / Q000378:metabolism* / Q000473:pathology; D003474:Curcumin / Q000008:administration & dosage* / Q000737:chemistry / Q000627:therapeutic use; D004337:Drug Carriers / Q000737:chemistry*; D015212:Inflammatory Bowel Diseases; D019804:Mesalamine / Q000008:administration & dosage* / Q000737:chemistry* / Q000627:therapeutic use; D011109:Polymethacrylic Acids / Q000737:chemistry*; D051381:Rats
chemical_list: D004337:Drug Carriers; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D019804:Mesalamine; D048271:Chitosan; D003474:Curcumin
keywords: Alginate; Colon-specific delivery; Inflammatory bowel disease; Mucoadhesive microparticulate; Thiolated chitosan