title: Development and evaluation of gastroretentive raft forming systems incorporating curcumin-Eudragit® EPO solid dispersions for gastric ulcer treatment.
abstract: Novel raft forming systems incorporating curcumin-Eudragit® EPO solid dispersions were developed to prolong the gastric residence time and provide for a controlled release therapy of curcumin to treat gastric ulcers. The solid dispersions of curcumin with Eudragit® EPO were prepared by the solvent evaporation method at various ratios to improve the solubility and the dissolution of curcumin. The optimum weight ratio of 1:5 for curcumin to Eudragit® EPO was used to incorporate into the raft forming systems. The raft forming formulations were composed of curcumin-Eudragit® EPO solid dispersions, sodium alginate as a gelling polymer and calcium carbonate for generating divalent Ca(2+) ions and carbon dioxide to form a floating raft. All formulations formed a gelled raft in 1min and sustained buoyancy on the 0.1N hydrochloric acid (pH 1.2) surface with a 60-85% release of curcumin within 8h. The curative effect on the acetic acid-induced chronic gastric ulcer in rats was determined. The curcumin raft forming formulations at 40mg/kg once daily showed a superior curative effect on the gastric ulcer in terms of the ulcer index and healing index than the standard antisecretory agent: lansoprazole (1mg/kg, twice daily) and a curcumin suspension (40mg/kg, twice daily). These studies demonstrated that the new raft forming systems containing curcumin solid dispersions are promising carriers for a stomach-specific delivery of poorly soluble lipophilic compounds.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand; Phytomedicine and Pharmaceutical Biotechnology Excellence Research Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand.
authors.forename: Nattha
authors.initials: N
authors.lastname: Kerdsakundee
authors.affiliation: Phytomedicine and Pharmaceutical Biotechnology Excellence Research Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand; Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand.
authors.forename: Sirima
authors.initials: S
authors.lastname: Mahattanadul
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand; Phytomedicine and Pharmaceutical Biotechnology Excellence Research Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand. Electronic address: ruedeekorn.w@psu.ac.th.
authors.forename: Ruedeekorn
authors.initials: R
authors.lastname: Wiwattanapatapee
mesh_terms: D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000627:therapeutic use; D003474:Curcumin / Q000008:administration & dosage* / Q000737:chemistry / Q000627:therapeutic use; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000379:methods; D065570:Gastric Absorption / Q000187:drug effects; D005753:Gastric Mucosa / Q000378:metabolism; D008297:Male; D011109:Polymethacrylic Acids / Q000737:chemistry*; D033362:Powder Diffraction; D017208:Rats, Wistar; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013270:Stomach / Q000187:drug effects*; D013276:Stomach Ulcer / Q000188:drug therapy*; D014783:Viscosity
chemical_list: D000897:Anti-Ulcer Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011109:Polymethacrylic Acids; C518398:Eudragit E PO; D003474:Curcumin
keywords: Curcumin; Gastric ulcers; Raft forming systems; Solid dispersions; Stomach-specific delivery