Polymorphic solidification of Linezolid confined in electrospun PCL fibers for controlled release in topical applications.
Poly(ϵ-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.
Department of Industrial Engineering, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy. Electronic address: loredana.ltammaro@unisa.it.
Loredana
L
Tammaro
Department of Pharmacy and Biomedical Science, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
Carmela
C
Saturnino
Department of Pharmacy and Biomedical Science, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
Sharon
S
D'Aniello
Department of Chemistry and Biology, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
Giovanni
G
Vigliotta
Department of Industrial Engineering, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
Vittoria
V
Vittoria
D000891:Anti-Infective Agents, Local / Q000737:chemistry* / Q000494:pharmacology; D003692:Delayed-Action Preparations / Q000737:chemistry* / Q000494:pharmacology; D065546:Drug Liberation; D000069349:Linezolid / Q000737:chemistry* / Q000494:pharmacology; D057139:Nanofibers / Q000737:chemistry*; D010599:Pharmacokinetics; D011091:Polyesters / Q000737:chemistry*; D013211:Staphylococcus aureus / Q000187:drug effects
D000891:Anti-Infective Agents, Local; D003692:Delayed-Action Preparations; D011091:Polyesters; C016240:polycaprolactone; D000069349:Linezolid
Antimicrobial Activity; Electrospinning; Linezolid; Nanofibers; Poly(ϵ-caprolactone)