4.4 Article

Dissolution Improvement of Electrospun Nanofiber-Based Solid Dispersions for Acetaminophen

期刊

AAPS PHARMSCITECH
卷 11, 期 2, 页码 809-817

出版社

SPRINGER
DOI: 10.1208/s12249-010-9438-4

关键词

drug-loaded nanofiber; electrospinning; microstructural characteristics; poorly water-soluble drug; solid dispersion

资金

  1. UK-CHINA Joint Laboratory for Therapeutic Textiles
  2. China Postdoctoral Science Foundation [200902195]
  3. Science and Technology Commission of Shanghai Municipality [08JC1400600]

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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 a parts per thousand 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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