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Polymorphic solidification of Linezolid confined in electrospun PCL fibers for controlled release in topical applications

TitoloPolymorphic solidification of Linezolid confined in electrospun PCL fibers for controlled release in topical applications
Tipo di pubblicazioneArticolo su Rivista peer-reviewed
Anno di Pubblicazione2015
AutoriTammaro, Loredana, Saturnino C., D'Aniello S., Vigliotta G., and Vittoria V.
RivistaInternational Journal of Pharmaceutics
Volume490
Paginazione32-38
ISSN03785173
Parole chiaveAnti-Infective Agents, antibacterial activity, article, bacterial cell, chemistry, controlled study, Crystallization, delayed release formulation, Delayed-Action Preparations, drug diffusion, drug effects, Drug Liberation, drug release, Electrospinning, in vitro study, linezolid, Local, Mechanics, microencapsulation, molecule, nanofiber, Nanofibers, nonhuman, pharmacokinetics, pharmacology, polycaprolactone, polyester, Polyesters, priority journal, Scanning electron microscopy, solid, Staphylococcus aureus, surface property, sustained drug release, Tensile Strength, topical antiinfective agent, ultraviolet spectrophotometry, X ray diffraction, Young modulus
Abstract

Poly(-caprolactone) (PCL) membranes loaded with Linezolid, chemically N-[[(5S)-3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide (empirical formula C16H20FN3O4) have been prepared by electrospinning technique, at different Linezolid concentrations (0.5, 1, 2.5 and 5%, w/w). Structural characterization, morphological analysis and the study of the mechanical properties have been performed on loaded membranes and compared with neat PCL membranes. Linezolid embedded in the membranes is prevalently amorphous, with a low crystallinity showing a different polymorphic form respect to the usual Form I and Form II. The release kinetics of the drug were studied by spectrophotometric analysis (UV-vis). It allowed to discriminate between Linezolid molecules on the surface and encapsulated into the fibers. The antibacterial activity of the electrospun membranes was effective to inhibit Staphylococcus aureus. The properties of the loaded membranes and their capability for local delivery of the antibiotic make them good candidates as drug release devices for topical use. © 2015 Elsevier B.V.All rights reserved.

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URLhttps://www.scopus.com/inward/record.uri?eid=2-s2.0-84929990052&doi=10.1016%2fj.ijpharm.2015.04.070&partnerID=40&md5=4ceb7f111a0a429299ab7405655c1b0d
DOI10.1016/j.ijpharm.2015.04.070
Citation KeyTammaro201532