title: Stomach specific polymeric low density microballoons as a vector for extended delivery of rabeprazole and amoxicillin for treatment of peptic ulcer.
abstract: The study was intended to develop a new intra-gastric floating in situ microballoons system for controlled delivery of rabeprazole sodium and amoxicillin trihydrate for the treatment of peptic ulcer disease. Eudragit S-100 and hydroxypropyl methyl cellulose based low density microballoons systems were fabricated by employing varying concentrations of Eudragit S-100 and hydroxypropyl methyl cellulose, to which varying concentrations of drug was added, and formulated by stirring at various speed and time to optimize the process and formulation variable. The formulation variables like concentration and ratio of polymers significantly affected the in vitro drug release from the prepared floating device. The validation of the gastro-retentive potential of the prepared microballoons was carried out in rabbits by orally administration of microballoons formulation containing radio opaque material. The developed formulations showed improved buoyancy and lower ulcer index as compared to that seen with plain drugs. Ulcer protective efficacies were confirmed in ulcer-bearing mouse model. In conclusion, greater compatibility, higher gastro-retention and higher anti-ulcer activity of the presently fabricated formulations to improve potential of formulation for redefining ulcer treatment are presented here. These learning exposed a targeted and sustained drug delivery potential of prepared microballoons in gastric region for ulcer therapeutic intervention as corroborated by in vitro and in vivo findings and, thus, deserves further attention for improved ulcer treatment.
authors: Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Central University, Sagar 470003, MP, India.
authors: Sandeep
authors: S
authors: Choudhary
authors: Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Central University, Sagar 470003, MP, India.
authors: Ashay
authors: A
authors: Jain
authors: Centre for Drug Delivery Research, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, Kuala Lumpur 50300, Malaysia.
authors: Mohd Cairul Iqbal Mohd
authors: MCIM
authors: Amin
authors: Pharmaceutical Nanotechnology Research Laboratory, Adina Institute of Pharmaceutical Sciences, MP 470002, India.
authors: Vijay
authors: V
authors: Mishra
authors: Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Central University, Sagar 470003, MP, India.
authors: Govind P
authors: GP
authors: Agrawal
authors: Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Central University, Sagar 470003, MP, India; Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201,USA. Electronic address: prashantdops@gmail.com.
authors: Prashant
authors: P
authors: Kesharwani
mesh_terms: D000658:Amoxicillin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D065546:Drug Liberation; D005753:Gastric Mucosa / Q000378:metabolism*; D008297:Male; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D010437:Peptic Ulcer / Q000188:drug therapy / Q000378:metabolism*; D011109:Polymethacrylic Acids / Q000737:chemistry*; D011817:Rabbits; D064750:Rabeprazole / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D013053:Spectrophotometry; D013270:Stomach / Q000187:drug effects / Q000473:pathology; D013997:Time Factors; D016896:Treatment Outcome
chemical_list: D000900:Anti-Bacterial Agents; D000897:Anti-Ulcer Agents; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D064750:Rabeprazole; D000658:Amoxicillin
keywords: Amoxicillin trihydrate; Buoyancy; Floating drug delivery system; Microballoons; Rabeprazole sodium