title: Fabrication, Physico-Chemical, and Pharmaceutical Characterization of Budesonide-Loaded Electrospun Fibers for Drug Targeting to the Colon.
abstract: The objective of this study was to fabricate and characterize electrospun fibers loaded with budesonide with the aim of controlling its release in the gastrointestinal tract. Budesonide is a nonhalogenated glucocorticosteroid drug, highly effective in the treatment of some inflammatory bowel diseases with local action throughout ileum and colon. At this aim, Eudragit® S 100, a polymer soluble at pH > 7, commonly used for enteric release of drugs, has been successfully spun into ultrafine fibers loaded with Budesonide (B) at 9% and 20% (w/w) using the electrospinning process. The physico-chemical characterization by scanning electron microscopy, X-ray diffraction, FTIR spectroscopy, and thermal analyses indicated the amorphous nature of budesonide in the electrospun systems. Dissolution rate measurements using a pH-change method showed negligible drug dissolved at pH 1.0 and sustained release at pH 7.2. Therefore, the pharmaceutical systems proposed, made of fibers, represent an effective method for drug targeting to terminal ileum and colon with the aim of improving the local efficacy of this drug.
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia 27100, Italy. Electronic address: giovanna.bruni@unipv.it.
authors.forename: Giovanna
authors.initials: G
authors.lastname: Bruni
authors.affiliation: Department of Drug Sciences, University of Pavia, Pavia, 27100, Italy.
authors.forename: Lauretta
authors.initials: L
authors.lastname: Maggi
authors.affiliation: Industrial Engineering Department, University of Salerno, Fisciano, Salerno 84084, Italy.
authors.forename: Loredana
authors.initials: L
authors.lastname: Tammaro
authors.affiliation: Department of Drug Sciences, University of Pavia, Pavia, 27100, Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Canobbio
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia 27100, Italy.
authors.forename: Rosadele
authors.initials: R
authors.lastname: Di Lorenzo
authors.affiliation: Industrial Engineering Department, University of Salerno, Fisciano, Salerno 84084, Italy.
authors.forename: Sharon
authors.initials: S
authors.lastname: D'aniello
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia 27100, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Domenighini
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia 27100, Italy.
authors.forename: Vittorio
authors.initials: V
authors.lastname: Berbenni
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia 27100, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Milanese
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia 27100, Italy.
authors.forename: Amedeo
authors.initials: A
authors.lastname: Marini
mesh_terms: D000893:Anti-Inflammatory Agents / Q000008:administration & dosage*; D019819:Budesonide / Q000008:administration & dosage*; D003106:Colon / Q000378:metabolism*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D016503:Drug Delivery Systems; D006801:Humans; D011109:Polymethacrylic Acids / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
chemical_list: D000893:Anti-Inflammatory Agents; D003692:Delayed-Action Preparations; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D019819:Budesonide
keywords: FTIR; amorphous; calorimetry (DSC); colonic drug delivery; dissolution; microscopy; polymer drug carrier