Plasticized Drug‐Loaded Melt Electrospun Polymer Mats: Characterization,Thermal Degradation,and Release Kinetics |
| |
| Institution: | 1. Organic Chemistry and Technology Department, Budapest University of Technology and Economics, Budapest H-1111, Hungary;2. Department of Inorganic and Analytical Chemistry, Budapest University of Technology and Economics, Budapest H-1111, Hungary;1. Institute of Chemical and Engineering Sciences, A*STAR (Agency for Science, Technology and Research), Jurong Island, Singapore 627833, Singapore;2. Division of Chemistry and Biological Chemistry, School of Physical and Mathematical Sciences, Nanyang Technological University, Singapore 637371, Singapore;3. Department of Laboratory Medicine, National University Hospital, Singapore 119074, Singapore;4. School of Materials Science and Engineering, Nanyang Technological University, Singapore 639798, Singapore;5. 5Advanced Drug Delivery Group, Faculty of Pharmacy, A15, The University of Sydney, Sydney, New South Wales 2006, Australia;6. Department of Chemical and Biomolecular Engineering, National University of Singapore, Singapore 117576, Singapore |
| |
| 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. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:1278–1287, 2014 |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
