title: Plasticized drug-loaded melt electrospun polymer mats: characterization, thermal degradation, and release kinetics.
abstract: Melt electrospinning (MES) was used to prepare fast dissolving fibrous drug delivery systems in the presence of plasticizers. This new method was found promising in the field of pharmaceutical formulation because it combines the advantages of melt extrusion and solvent-based electrospinning. Lowering of the process temperature was performed using plasticizers in order to avoid undesired thermal degradation. Carvedilol (CAR), a poorly water-soluble and thermal-sensitive model drug, was introduced into an amorphous methacrylate terpolymer matrix, Eudragit® E, suitable for fiber formation. Three plasticizers (triacetin, Tween® 80, and polyethylene glycol 1500) were tested, all of which lowered the process temperature effectively. Scanning electron microscopy, X-ray diffraction, differential scanning calorimetry, and Raman microspectrometry investigations showed that crystalline CAR turned into an amorphous form during processing and preserved it for longer time. In vitro dissolution studies revealed ultrafast drug dissolution of the fibrous samples. According to the HPLC impurity tests, the reduced stability of CAR under conditions applied without plasticizer could be avoided using plasticizers, whereas storage tests also indicated the importance of optimizing the process parameters during MES.
authors.affiliation: Organic Chemistry and Technology Department, Budapest University of Technology and Economics, Budapest, H-1111, Hungary.
authors.forename: Attila
authors.initials: A
authors.lastname: Balogh
authors.forename: Gábor
authors.initials: G
authors.lastname: Drávavölgyi
authors.forename: Kornél
authors.initials: K
authors.lastname: Faragó
authors.forename: Attila
authors.initials: A
authors.lastname: Farkas
authors.forename: Tamás
authors.initials: T
authors.lastname: Vigh
authors.forename: Péter Lajos
authors.initials: PL
authors.lastname: Sóti
authors.forename: István
authors.initials: I
authors.lastname: Wagner
authors.forename: János
authors.initials: J
authors.lastname: Madarász
authors.forename: Hajnalka
authors.initials: H
authors.lastname: Pataki
authors.forename: György
authors.initials: G
authors.lastname: Marosi
authors.forename: Zsombor Kristóf
authors.initials: ZK
authors.lastname: Nagy
mesh_terms: D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000737:chemistry; D002227:Carbazoles / Q000008:administration & dosage* / Q000737:chemistry; D000077261:Carvedilol; D016503:Drug Delivery Systems; D004355:Drug Stability; D010968:Plasticizers / Q000737:chemistry*; D011109:Polymethacrylic Acids / Q000737:chemistry*; D011412:Propanolamines / Q000008:administration & dosage* / Q000737:chemistry; D012995:Solubility; D013696:Temperature
chemical_list: D000959:Antihypertensive Agents; D002227:Carbazoles; D010968:Plasticizers; D011109:Polymethacrylic Acids; D011412:Propanolamines; D000077261:Carvedilol; C038300:methylmethacrylate-methacrylic acid copolymer
keywords: HPLC; Raman spectroscopy; amorphous; enhanced dissolution rate; extrusion; melt electrospinning; oral drug delivery; plasticizer; solid dispersion; viscosity