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

Paper ID Volume ID Publish Year Pages File Format Full-Text
28 4 2016 10 PDF Available
Title
Electrospun pH-sensitive core–shell polymer nanocomposites fabricated using a tri-axial process
Abstract

A modified tri-axial electrospinning process was developed for the generation of a new type of pH-sensitive polymer/lipid nanocomposite. The systems produced are able to promote both dissolution and permeation of a model poorly water-soluble drug. First, we show that it is possible to run a tri-axial process with only one of the three fluids being electrospinnable. Using an electrospinnable middle fluid of Eudragit S100 (ES100) with pure ethanol as the outer solvent and an unspinnable lecithin-diclofenac sodium (PL–DS) core solution, nanofibers with linear morphology and clear core/shell structures can be fabricated continuously and smoothly. X-ray diffraction proved that these nanofibers are structural nanocomposites with the drug present in an amorphous state. In vitro dissolution tests demonstrated that the formulations could preclude release in acidic conditions, and that the drug was released from the fibers in two successive steps at neutral pH. The first step is the dissolution of the shell ES100 and the conversion of the core PL–DS into sub-micron sized particles. This frees some DS into solution, and later the remaining DS is gradually released from the PL–DS particles through diffusion. Ex vivo permeation results showed that the composite nanofibers give a more than twofold uplift in the amount of DS passing through the colonic membrane as compared to pure DS; 74% of the transmitted drug was in the form of PL–DS particles. The new tri-axial electrospinning process developed in this work provides a platform to fabricate structural nanomaterials, and the core–shell polymer-PL nanocomposites we have produced have significant potential applications for oral colon-targeted drug delivery.Statement of SignificanceA modified tri-axial electrospinning is demonstrated to create a new type of core–shell pH-sensitive polymer/lipid nanocomposites, in which an electrospinnable middle fluid is exploited to support the un-spinnable outer and inner fluids. The structural nanocomposites are able to provide a colon-targeted sustained release and an enhanced permeation performance of diclofenac sodium. The developed tri-axial process can provide a platform for fabricating new structural nanomaterials with high quality. The strategy of a combined usage of polymeric excipients and phospholipid in a core–shell format should provide new possibilities of developing novel drug delivery systems for efficacious oral administration of poorly-water soluble drugs.

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Keywords
Tri-axial electrospinning; Core-sheath fibers; Polymer–lipid nanocomposites; Colon-targeted drug delivery; Electrospinnability
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Electrospun pH-sensitive core–shell polymer nanocomposites fabricated using a tri-axial process
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Publisher
Database: Elsevier - ScienceDirect
Journal: Acta Biomaterialia - Volume 35, 15 April 2016, Pages 77–86
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us