Abstract

This study reports a new type of drug-loaded core-shell nanofibers capable of providing dual controlled release with tunable dose in the second phase. The core-shell nanofibers were fabricated through a modified coaxial electrospinning using a Teflon-coated concentric spinneret. Poly(vinyl pyrrolidone) and ethyl cellulose were used as the shell and core polymer matrices respectively, and the content of active ingredient acetaminophen (APAP) in the core was programmed. The Teflon-coated concentric spinneret may facilitate the efficacious and stable preparation of core-shell nanofibers through the modified coaxial electrospinning, where the core fluids were electrospinnable and the shell fluid had no electrospinnability. The resultant nanofibers had linear morphologies and clear core-shell structures, as observed by the scanning and transmission electron microscopic images. APAP was amorphously distributed in the shell and core polymer matrices due to the favorite second-order interactions, as indicated by the X-ray diffraction and FTIR spectroscopic tests. The results from the in vitro dissolution tests demonstrated that the core-shell nanofibers were able to furnish the desired dual drug controlled-release profiles with a tunable drug release amount in the second phase. The modified coaxial electrospinning is a useful tool to generate nanostructures with a tailored components and compositions in their different parts, and thus to realize the desired functional performances.

Highlights

  • Electrospinning, a simple and straightforward top-down process for generating nanofibers, has drawn increasing attentions due to easy implementation, capability of treating a variety of materials, convenience in obtaining composites of multiple components and a wide variety potential applications of the resultant nanofibers [1,2,3,4,5,6]

  • Shell fluid consists of 15% (w/v) poly(vinyl pyrrolidone) (PVP) K25 and a fixed APAP concentration of 5% (w/v) in a mixture of ethanol and DMAc (8:2, v:v); b Core fluid consists of 24% (w/v) ethyl cellulose (EC) and a varied concentration of APAP in ethanol; c “Linear” morphology refers to nanofibers with few beads or spindles and “Mixed” morphology to nanofibers exhibiting beads-on-a-string or spindles-on-a-string features; d The theoretical value (w/w) in the solid nanofibers calculated according to the shell and core fluid flow rates and the drug content in the shell and core solutions

  • A modified coaxial electrospinning was carried out to prepare core-shell nanofibers that provided dual drug release profiles of APAP, and the drug contents in the core fluids were successfully exploited as a tool to tailor the dose of drug released in the second phase

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Summary

Introduction

Electrospinning, a simple and straightforward top-down process for generating nanofibers, has drawn increasing attentions due to easy implementation, capability of treating a variety of materials, convenience in obtaining composites of multiple components and a wide variety potential applications of the resultant nanofibers [1,2,3,4,5,6]. Advanced technologies (such as three-dimensional printing and nanotechniques [22,23]) are continuously investigated in the literature in order to produce novel materials or DDS for providing dual release, taking its advantage in a more accurate time-programmed administration of API and fulfilling the specific therapeutic needs of some diseases. Electrospinning can achieve this objective through strategies such as preparing multi-layered nanofiber mats using a sequential single fluid process or producing fibers containing drug-loaded nanoparticles through the electrospinning of suspensions [23]. Using poly(vinyl pyrrolidone) (PVP) and ethyl cellulose (EC) as the shell and core polymer matrices, and acetaminophen (APAP, a common NSAID) as the model API, a modified coaxial electrospinning with a Teflon-coated concentric spinneret was conducted for the preparation of core-shell drug-loaded nanofibers, in which the shell fluid was un-spinnable

Results and Discussion
Morphology and Structure of Nanofibers
Physical Status and Compatibility of Components
Dual Release Profiles with Tunable Dose in the Second Phase
Materials
Modified Coaxial Electrospinning
Morphology
Physical Status and Compatibility
In Vitro Dissolution Tests
Conclusions
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