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Electrospun pH-sensitive core-shell polymer nanocomposites fabricated using a tri-axial process.

Chen Yang1, Deng-Guang Yu1, Deng Pan1

  • 1School of Materials Science & Engineering, University of Shanghai for Science and Technology, 516 Jungong Road, Shanghai 200093, China.

Acta Biomaterialia
|February 24, 2016
PubMed
Summary

A novel tri-axial electrospinning technique created pH-sensitive polymer/lipid nanocomposites for enhanced colon-targeted drug delivery. These core-shell structures improve dissolution and permeation of poorly water-soluble drugs like diclofenac sodium.

Keywords:
Colon-targeted drug deliveryCore-sheath fibersElectrospinnabilityPolymer–lipid nanocompositesTri-axial electrospinning

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Area of Science:

  • Materials Science
  • Nanotechnology
  • Pharmaceutics

Background:

  • Developing effective drug delivery systems for poorly water-soluble drugs remains a challenge.
  • Colon-targeted delivery can improve therapeutic efficacy and reduce systemic side effects.
  • Nanocomposite materials offer unique properties for drug delivery applications.

Purpose of the Study:

  • To develop a modified tri-axial electrospinning process for creating pH-sensitive polymer/lipid nanocomposites.
  • To evaluate the potential of these nanocomposites for colon-targeted delivery and enhanced permeation of diclofenac sodium.
  • To demonstrate the fabrication of linear nanofibers with clear core-shell structures.

Main Methods:

  • Utilized a modified tri-axial electrospinning process with Eudragit S100 as the electrospinnable middle fluid.
  • Fabricated core-shell nanofibers containing lecithin-diclofenac sodium (PL-DS) in the core and Eudragit S100 in the shell.
  • Characterized the nanofibers using X-ray diffraction to confirm their structure and amorphous drug state.
  • Performed in vitro dissolution tests at acidic and neutral pH.
  • Conducted ex vivo permeation studies across a colonic membrane.

Main Results:

  • Successfully fabricated linear, core-shell nanofibers using a tri-axial electrospinning process with only one electrospinnable fluid.
  • Nanocomposites showed pH-sensitive behavior, preventing drug release in acidic conditions and enabling two-step release at neutral pH.
  • Ex vivo studies demonstrated a twofold increase in diclofenac sodium permeation through the colonic membrane compared to the pure drug.
  • 74% of the permeated drug was found in the form of lecithin-diclofenac sodium particles.

Conclusions:

  • A modified tri-axial electrospinning method enables the creation of high-quality, core-shell pH-sensitive polymer/lipid nanocomposites.
  • These nanocomposites facilitate colon-targeted sustained release and enhanced permeation of diclofenac sodium.
  • This approach offers a promising platform for developing novel oral drug delivery systems for poorly water-soluble drugs.