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Fabrication, Physico-Chemical, and Pharmaceutical Characterization of Budesonide-Loaded Electrospun Fibers for Drug Targeting to the Colon

TitleFabrication, Physico-Chemical, and Pharmaceutical Characterization of Budesonide-Loaded Electrospun Fibers for Drug Targeting to the Colon
Publication TypeArticolo su Rivista peer-reviewed
Year of Publication2015
AuthorsBruni, G., Maggi L., Tammaro Loredana, Canobbio A., Di Lorenzo R., D'Aniello S., Domenighini C., Berbenni V., Milanese C., and Marini A.
JournalJournal of Pharmaceutical Sciences
Volume104
Pagination3798-3803
ISSN00223549
KeywordsAnti-Inflammatory Agents, antiinflammatory agent, article, budesonide, chemistry, colon, controlled drug release, delayed release formulation, Delayed-Action Preparations, Differential scanning calorimetry, drug delivery system, Drug Delivery Systems, drug solubility, drug targeting, Electrospinning, eudragit, Fourier Transform Infrared, gastrointestinal tract, human, Humans, ileum, infrared spectroscopy, metabolism, methacrylic acid methyl ester, methylmethacrylate-methacrylic acid copolymer, particle size, pH, physical chemistry, polymethacrylic acid derivative, Polymethacrylic Acids, Scanning electron microscopy, simulation, Solubility, Spectroscopy, sustained drug release, thermal analysis, thermogravimetry, X ray diffraction, X ray powder diffraction, X-Ray Diffraction
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. © 2015 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 104:3798-3803, 2015 © 2015 Wiley Periodicals, Inc. and the American Pharmacists Association.

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URLhttps://www.scopus.com/inward/record.uri?eid=2-s2.0-84944149735&doi=10.1002%2fjps.24587&partnerID=40&md5=ef2f6ad39cf288554227ad1e2e6bb32b
DOI10.1002/jps.24587
Citation KeyBruni20153798