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Dissolution Improvement of Electrospun Nanofiber-Based Solid Dispersions for Acetaminophen
Authors:Deng-Guang Yu  Christopher Branford-White  Kenneth White  Xue-Lian Li  Li-Min Zhu
Institution:(1) College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, 2999 North Renmin Road, Songjiang District, Shanghai, 201620, China;(2) Institute for Health Research and Policy, London Metropolitan University, London, N7 8DB, UK;
Abstract:The objective of the present investigation was to prepare novel solid dispersions (SDs) of poorly water-soluble drugs with special microstructural characteristics using electrospinning process. With the hydrophilic polymer polyvinylpyrrolidone as the filament-forming polymer and acetaminophen (APAP) as the poorly water-soluble drug model, SDs having a continuous web structure, and in the form of non-woven nanofiber membranes, were successfully prepared. The electrospun nanofiber-based SDs were compared with those prepared from three traditional SD processes such as freeze-drying, vacuum drying, and heating drying. The surface morphologies, the drug physical status, and the drug-polymer interactions were investigated by scanning electron microscopy, differential scanning calorimetry, X-ray diffraction, and attenuated total reflectance Fourier transform infrared. In vitro dissolution tests demonstrated that the electrospun nanofibers released 93.8% of the APAP content in the first 2 minutes and that the dissolution rates of APAP from the different SDs had the following order: electrospun membrane > vacuum-dried membrane ≈ freeze-dried membrane > heat-dried membrane. Electrospun nanofiber-based SDs showed markedly better dissolution-improving effects than the other SDs, mainly due to their huge surface area, high porosity resulting from web structure, and the more homogeneous distribution of APAP in the nanofiber matrix.
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