title: Site Targeted Press Coated Delivery of Methylprednisolone Using Eudragit RS 100 and Chitosan for Treatment of Colitis.
abstract: BACKGROUND
  Inflammatory bowel disease (IBD) is one of the five most prevalent gastrointestinal disease burdens which commonly require lifetime care. Worldwide incidence rate of ulcerative colitis and Crohn's disease is about 16.8% and 13.4% respectively. Colitis is an inflammation of the colon. Colon targeted drug delivery will direct the drug to the colon. The drug will reach at the site of action and hence its side effects as well as dose can be reduced. Recent patent describes treatment of ulcerative colitis using anti CD3 antibodies, with nicotine and anti-depressant drugs, budesonide foam etc.
  
  
  OBJECTIVE
  Present study deals with optimization of site targeted methylprednisolone delivery for treatment of colitis.
  
  
  METHODS
  Chitosan and Eudragit RS 100 were used as coating polymers. Tablets were prepared by press coated technology. The core tablets contain drug, avicel as binder, croscarmellose sodium as super disintegrant and dicalcium phosphate as diluent. Drug excipient compatibility was carried out using FTIR, UV and DSC. Design of experiment was used to optimize the formulation. Tablets were evaluated for thickness, weight variation, hardness, swelling index, in-vitro drug release and release of drug in simulated media.
  
  
  RESULTS
  Optimized batch (B2) contained chitosan 40% and eudragit RS 100 17.5%. B2 showed in-vitro drug release 85.65 ± 7.6% in 6.8 pH phosphate buffer and 96.7 ±9.1% in simulated media after 7.5 hours.
  
  
  CONCLUSIONS
  In-vivo x-ray placebo study for formulation B2 had shown that the tablet reached to the ascending colon after 5 hours. This indicated a potential site targeted delivery of optimized batch B2.
authors.affiliation: Department of Pharmaceutics, MAEER's Maharashtra Institute of Pharmacy, MIT Campus, Pune, (MS), 411038, India. swati.jagdale@mippune.edu.in.
authors.forename: Swati
authors.initials: S
authors.lastname: Jagdale
authors.forename: Apoorva
authors.initials: A
authors.lastname: Chandekar
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry*; D000284:Administration, Oral; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D048271:Chitosan / Q000737:chemistry*; D003092:Colitis / Q000188:drug therapy*; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D005765:Gastrointestinal Agents / Q000008:administration & dosage / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D008775:Methylprednisolone / Q000008:administration & dosage / Q000737:chemistry*; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D017550:Spectroscopy, Fourier Transform Infrared; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D000180:Acrylic Resins; D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D005765:Gastrointestinal Agents; D013607:Tablets; C050528:Eudragit RS; D048271:Chitosan; D008775:Methylprednisolone