title: Floating-bioadhesive gastroretentive Caesalpinia pulcherrima-based beads of amoxicillin trihydrate for Helicobacter pylori eradication.
abstract: BACKGROUND
  An oral dosage form containing floating bioadhesive gastroretentive microspheres forms a stomach-specific drug delivery system for the treatment of Helicobacter pylori.
  
  
  OBJECTIVE
  To prepare and evaluate controlled release floating bioadhesive gastroretentive chitosan-coated amoxicillin trihydrate-loaded Caesalpinia pulcherrima galactomannan (CPG)-alginate beads (CCA-CPG-A), for H. pylori eradication.
  
  
  METHODS
  CCA-CPG-A beads were prepared by ionotropic gelation, using 2(3) factorial design with quantity of drug, combination of CPG with sodium alginate and concentration of calcium chloride as variables. Beads facilitated mucoadhesion to gastric mucosa with floating nature caused by chitosan coating for wide distribution throughout GIT. Developed beads were evaluated for characteristics like beads size-morphology, entrapment efficiency, DSC, XRD, FTIR, swelling ratio, in vitro mucoadhesion, in vitro drug release, in vitro floating and in vitro H. pylori growth inhibition studies. CCA-CPG-A beads were studied in Wistar rats for in vivo gastric mucoadhesion, in vivo H. pylori growth inhibition studies using PCR amplification of isolated DNA, rapid urease test.
  
  
  RESULTS
  Developed beads possess drug release of 79-92%, entrapment efficiency of 65-89%, mucoadhesion of 61-89%. In vivo mucoadhesion study showed more than 85% mucoadhesion of beads even after 7th hour. In vitro-in vivo growth inhibition study showed complete eradication of H. pylori.
  
  
  CONCLUSIONS
  CPG-alginate and chitosan in beads interacts with gastric mucosubstrate surface for prolonged gastric residence with floating bioadhesion mechanism for H. pylori eradication in rats.
  
  
  CONCLUSIONS
  Floating bioadhesive CCA-CPG-A beads offer a promising drug delivery system for H. pylori eradication at lower dose, reduced adverse effect and enhance bioavailability.
authors.affiliation: a Department of Pharmaceutics , M.E.T.'s Institute of Pharmacy , Nasik , Maharashtra , India.
authors.forename: Nilima A
authors.initials: NA
authors.lastname: Thombre
authors.affiliation: a Department of Pharmaceutics , M.E.T.'s Institute of Pharmacy , Nasik , Maharashtra , India.
authors.forename: Paraag S
authors.initials: PS
authors.lastname: Gide
mesh_terms: D000268:Adhesiveness; D000284:Administration, Oral; D000464:Alginates / Q000737:chemistry*; D000658:Amoxicillin / Q000008:administration & dosage* / Q000737:chemistry; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry; D001682:Biological Availability; D029911:Caesalpinia / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D048271:Chitosan / Q000737:chemistry; D018360:Crystallography, X-Ray; D003692:Delayed-Action Preparations; D004195:Disease Models, Animal; D004304:Dosage Forms; D004337:Drug Carriers; D004339:Drug Compounding; D005260:Female; D005690:Galactose / Q000031:analogs & derivatives; D005753:Gastric Mucosa / Q000378:metabolism*; D020723:Glucuronic Acid / Q000737:chemistry; D016481:Helicobacter Infections / Q000188:drug therapy* / Q000382:microbiology; D016480:Helicobacter pylori / Q000187:drug effects* / Q000254:growth & development; D006603:Hexuronic Acids / Q000737:chemistry; D007700:Kinetics; D008297:Male; D008351:Mannans / Q000737:chemistry* / Q000302:isolation & purification / Q000378:metabolism; D008956:Models, Chemical; D010316:Particle Size; D033362:Powder Diffraction; D017208:Rats, Wistar; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D000464:Alginates; D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D004304:Dosage Forms; D004337:Drug Carriers; D006603:Hexuronic Acids; D008351:Mannans; C012990:galactomannan; D000658:Amoxicillin; D020723:Glucuronic Acid; D048271:Chitosan; D005690:Galactose
keywords: Amoxicillin trihydrate; Helicobacter pylori; beads Caesalpinia pulcherrima galactomannan; gastroretentive