Abstract

The present study reports a new type of sedative nanofiber membranes that were developed to permit very rapid oral delivery of helicid with concomitant taste masking. A coaxial electrospinning process was exploited to prepare core–shell nanofibers and to control the spatial depositions of different functional components. A series of tests was undertaken to characterize the resultant nanofibers. Following optimization of the electrospinning parameters, two types of core–shell nanofibers with average diameters of 730 ± 140 and 770 ± 160 nm were successfully prepared. These had uniform linear morphologies and clear core–shell structures, as verified by scanning and transmission electron microscopy images. The fibers contained sucralose in the shell and helicid in the core; X-ray diffraction demonstrated that both functional components were present in the amorphous physical form. There is significant hydrogen bonding between the functional components and the poly(vinylpyrrolidone) used as the carrier matrix, as shown from Fourier transform infrared spectroscopy and molecular mechanics simulations. In vitro dissolution tests showed that the formulations were able to release the entire incorporated drug extremely rapidly (within 1 min) when they encountered a dissolution medium, whereas the commercially available product released only 13.4 % of its drug loading in the same time. By tailoring the distribution of functional ingredients in electrospun core–shell structures, new drug delivery systems which can both accelerate dissolution and also mask unpleasant tastes were produced.

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