title: Budesonide Loaded PLGA Nanoparticles for Targeting the Inflamed Intestinal Mucosa--Pharmaceutical Characterization and Fluorescence Imaging.
abstract: OBJECTIVE
  The purpose of this study was to evaluate the specifically targeted efficiency of budesonide loaded PLGA nanoparticles for the treatment of inflammatory bowel disease (IBD).
  
  
  METHODS
  The nanoparticles were prepared by an oil/water (O/W) emulsion evaporation technique. The nanoparticles were characterized for their size, shape and in vitro drug release profile. Solid state characterization was carried out by differential scanning calorimetry (DSC) and X-ray Power diffraction (XPRD). In order to evaluate the targeted efficiency of nanoparticles, a particle localization study in the healthy and in the inflamed colon was determined in vivo. These data were complemented by cryo-sections.
  
  
  RESULTS
  Nanoparticles were 200 ± 05 nm in size with a smooth and spherical shape. The encapsulation efficiency was around 85 ± 3.5%, which was find-out by both, direct and indirect methods. Release of budesonide from the nanoparticles showed a biphasic release profile with an initial burst followed by sustained release. XPRD data revealed that the drug in the polymer matrix existed in crystalline state. Nanoparticles accumulation in inflamed tissues was evaluated by in-vivo imaging system and it was found that particles are accumulated in abundance at the site of inflammation when compared to the healthy group.
  
  
  CONCLUSIONS
  The study demonstrates that the budesonide loaded PLGA nanoparticles are an efficient delivery system for targeted drug delivery to the inflamed intestinal mucosa.
authors.affiliation: Department of Pharmacy, Quaid-i-Azam University, Islamabad, 45320, Pakistan.|Biopharmaceutics and Pharmaceutical Technology, Saarland University, Campus A4.1, 66123, Saarbrücken, Germany.
authors.forename: Hussain
authors.initials: H
authors.lastname: Ali
authors.affiliation: Medical Clinic I, University Hospital Erlangen, Research Campus, 91052, Erlangen, Germany.
authors.forename: Benno
authors.initials: B
authors.lastname: Weigmann
authors.affiliation: Department of Drug Delivery (DDEL), Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Saarland University, Campus E 8.1, 66123, Saarbrücken, Germany.
authors.forename: Eva-Maria
authors.initials: EM
authors.lastname: Collnot
authors.affiliation: Department of Pharmacy, Kohat University of Science and Technology, Kohat, KPK, Pakistan.
authors.forename: Saeed Ahmad
authors.initials: SA
authors.lastname: Khan
authors.affiliation: Biopharmaceutics and Pharmaceutical Technology, Saarland University, Campus A4.1, 66123, Saarbrücken, Germany.|Department of Drug Delivery (DDEL), Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Saarland University, Campus E 8.1, 66123, Saarbrücken, Germany.
authors.forename: Maike
authors.initials: M
authors.lastname: Windbergs
authors.affiliation: Biopharmaceutics and Pharmaceutical Technology, Saarland University, Campus A4.1, 66123, Saarbrücken, Germany. claus-michael.lehr@helmholtz-hzi.de.|Department of Drug Delivery (DDEL), Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Saarland University, Campus E 8.1, 66123, Saarbrücken, Germany. claus-michael.lehr@helmholtz-hzi.de.
authors.forename: Claus-Michael
authors.initials: CM
authors.lastname: Lehr
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D019819:Budesonide / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D003092:Colitis / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D065546:Drug Liberation; D006801:Humans; D015212:Inflammatory Bowel Diseases / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism* / Q000473:pathology; D019344:Lactic Acid / Q000737:chemistry*; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D061848:Optical Imaging; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D014961:X-Ray Diffraction
chemical_list: D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D019819:Budesonide
keywords: DSC; XRD; budesonide; colitis; nanoparticles; oxazolone; sustained drug release