title: Solvent-free melt electrospinning for preparation of fast dissolving drug delivery system and comparison with solvent-based electrospun and melt extruded systems.
abstract: The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit® E type was used as a fiber forming polymer matrix. For comparison, ethanol-based electrospinning and melt extrusion (EX) methods were used to produce samples that had the same composition as the melt electrospun system. According to the results of scanning electron microscopy, X-ray diffraction, differential scanning calorimetry, and Fourier transformed infrared spectrometry investigations, amorphous solid nanodispersions/solutions of CAR in Eudragit® E matrix were obtained in all cases with 20 m/m % drug content. In vitro drug release in acidic media from the extrudates was significantly faster (5 min) than that from crystalline CAR. Moreover, ultrafast drug release was achieved from the solvent-free melt and ethanol-based electrospun samples because of their huge surface area and the soluble polymer matrix in the acidic media. These results demonstrate that solvent-free MES is a promising, novel technique for the production of drug delivery systems with enhanced dissolution because it can combine the advantages of EX (e.g., solvent-free, continuous process, and effective amorphization) and solvent-based electrospinning (huge product surface area).
authors.affiliation: Organic Chemistry and Technology Department, Budapest University of Technology and Economics, Budapest H-1111, Hungary. zsknagy@oct.bme.hu
authors.forename: Zsombor Kristóf
authors.initials: ZK
authors.lastname: Nagy
authors.forename: Attlia
authors.initials: A
authors.lastname: Balogh
authors.forename: Gábor
authors.initials: G
authors.lastname: Drávavölgyi
authors.forename: James
authors.initials: J
authors.lastname: Ferguson
authors.forename: Hajnalka
authors.initials: H
authors.lastname: Pataki
authors.forename: Balázs
authors.initials: B
authors.lastname: Vajna
authors.forename: György
authors.initials: G
authors.lastname: Marosi
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods*; D016503:Drug Delivery Systems / Q000379:methods*; D012995:Solubility; D012997:Solvents / Q000008:administration & dosage / Q000138:chemical synthesis*; D013997:Time Factors; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D012997:Solvents