Special Issue "Electrospun and Electrosprayed Formulations for Drug Delivery"

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: 30 November 2018

Special Issue Editors

Guest Editor
Dr Ian S. Blagbrough

Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK
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Interests: electrospinning; electrospraying; biopolymers; coaxial; controlled drug delivery; nanofibre; polymer therapeutics; sustained release; tissue engineering; wound healing; biodegradable; gene therapy; polycaprolactone
Guest Editor
Dr Gareth R. Williams

UCL School of Pharmacy, University College London, 29 - 39 Brunswick Square, London WC1N 1AX, UK
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Fax: +44 207 753 5942
Interests: multi-fluid electrospinning; modified release formulations; targeted drug delivery; theranostics; adjuvants

Special Issue Information

Dear Colleagues,

Electrospinning and spraying have been widely explored to prepare drug delivery systems. In this research, it is important to demonstrate the biocompatibility of the electrospun matrices and to investigate the biological activity of the delivered drug or growth factor. The latter must be maintained and the drug delivered in a controlled manner to prepare potent new medicines. Sustained and controlled release of active pharmaceutical ingredients (API) from drug-loaded electrospun matrices can be achieved, with systems composed of biopolymers or biocompatible synthetic polymers found to demonstrate compatibility with human cells as well as significant biological activity.

Investigations of a wide range of polymers and their blends have been undertaken in order to produce advanced materials, potentially displaying superior rheological and viscoelastic properties over other polymers. Different electrospinning techniques allow for the loading of a range of drugs with high encapsulation efficiencies. The potential applications of electrospun nanofibres include drug delivery in research areas as diverse as anti-cancer therapeutics, gene therapy, and wound healing, as post-surgical abdominal anti-adhesion products, and for tissue engineering. Electrospun nanofibres have a large surface area and can mimic the topographical features of extracellular matrices (ECM). Materials with such properties are potentially useful for the much-needed production of bioactive scaffolds, combining the controlled release of a wide variety of therapeutically active agents (e.g. antibiotics, anti-cancer drugs, growth factors, DNA) with a nanofibrous scaffold which will support cell proliferation (e.g. in tissue engineering) or prevent cell migration. With controlled release of the entrapped API and models available both in vitro and in vivo to establish viability in target cells, successful drug delivery can be quantified and cell morphology and pathology assessed, especially aiming for minimal off-target effects.

The simplest electrospun drug delivery system is comprised of only a blend of polymer and drug. However, more advanced materials such as double- and triple-layered fibrous dressings and implants can be produced by electrospinning, representing a significant shift in how we view drug delivery technology.

Despite their great promise, there is more research still to be done before these formulations can be taken forward into the clinic. The controlled release profiles of electrospun matrices and their biocompatibility need to be clearly established.

This special issue of Pharmaceutics has a clear focus on research in these important areas.

Dr Ian S. Blagbrough
Dr Gareth R. Williams
Guest Editors

Manuscript Submission Information

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Keywords

  • Electrospinning
  • Electrohydrodynamic
  • Controlled release
  • Polymer formulations
  • Biopolymer formulations

Published Papers (3 papers)

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Research

Open AccessArticle Fast Dissolving of Ferulic Acid via Electrospun Ternary Amorphous Composites Produced by a Coaxial Process
Pharmaceutics 2018, 10(3), 115; https://doi.org/10.3390/pharmaceutics10030115
Received: 30 May 2018 / Revised: 23 July 2018 / Accepted: 24 July 2018 / Published: 2 August 2018
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Abstract
Enhancing the dissolution of insoluble active ingredients comprises one of the most important issues in the pharmaceutical and biomaterial fields. Here, a third generation solid dispersion (3rd SD) of ferulic acid was designed and fabricated by a modified coaxial electrospinning process. A traditional
[...] Read more.
Enhancing the dissolution of insoluble active ingredients comprises one of the most important issues in the pharmaceutical and biomaterial fields. Here, a third generation solid dispersion (3rd SD) of ferulic acid was designed and fabricated by a modified coaxial electrospinning process. A traditional second generation SD (2nd SD) was also prepared by common one-fluid blending electrospinning and was used as a control. With poly(vinyl alcohol) as the fiber matrix and polyvinylpyrrolidone K10 as an additive in the 3rd SDs, the two electrospinning processes were investigated. The prepared 2nd and 3rd SDs were subjected to a series of characterizations, including X-ray diffraction (XRD), scanning electron microscope (SEM), hydrophilicity and in vitro drug dissolving experiments. The results demonstrate that both SDs were monolithic nanocomposites and that the drugs were amorphously distributed within the matrix. However, the 3rd SDs had better morphology with smaller size, narrower size distribution, and smaller water contact angles than the 2nd SDs. Dissolution tests verified that the 3rd SDs could release their loaded cargoes within 60 s, which was over three times faster than the 2nd SDs. Therefore, a combined strategy based on the modified coaxial electrospinning and the logical selections of drug carriers is demonstrated for creating advanced biomaterials. Full article
(This article belongs to the Special Issue Electrospun and Electrosprayed Formulations for Drug Delivery)
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Graphical abstract

Open AccessArticle Homogenization of Amorphous Solid Dispersions Prepared by Electrospinning in Low-Dose Tablet Formulation
Pharmaceutics 2018, 10(3), 114; https://doi.org/10.3390/pharmaceutics10030114
Received: 15 June 2018 / Revised: 23 July 2018 / Accepted: 23 July 2018 / Published: 2 August 2018
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Abstract
Low-dose tablet formulations were produced with excellent homogeneity based on drug-loaded electrospun fibers prepared by single-needle as well as scaled-up electrospinning (SNES and HSES). Carvedilol (CAR), a BCS II class compound, served as the model drug while poly (vinylpyrrolidone-co-vinyl acetate) (PVPVA64)
[...] Read more.
Low-dose tablet formulations were produced with excellent homogeneity based on drug-loaded electrospun fibers prepared by single-needle as well as scaled-up electrospinning (SNES and HSES). Carvedilol (CAR), a BCS II class compound, served as the model drug while poly (vinylpyrrolidone-co-vinyl acetate) (PVPVA64) was adopted as the fiber-forming polymer. Scanning electron microscopy (SEM) imaging was used to study the morphology of HSES and SNES samples. Different homogenization techniques were compared to maximize homogeneity: mixing in plastic bags and in a high-shear granulator resulting in low-shear mixing (LSM) and high-shear mixing (HSM). Drug content and homogeneity of the tablets were measured by UV-Vis spectrometry, the results revealed acceptably low-dose fluctuations especially with formulations homogenized with HSM. Sieve analysis was used on the final LSM and HSM powder mixtures in order to elucidate the observed differences between tablet homogeneity. Tablets containing drug-loaded electrospun fibers were also studied by Raman mapping demonstrating evenly distributed CAR within the corpus. Full article
(This article belongs to the Special Issue Electrospun and Electrosprayed Formulations for Drug Delivery)
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Graphical abstract

Open AccessArticle The Effect of Molecular Properties on Active Ingredient Release from Electrospun Eudragit Fibers
Pharmaceutics 2018, 10(3), 103; https://doi.org/10.3390/pharmaceutics10030103
Received: 16 March 2018 / Revised: 11 May 2018 / Accepted: 16 May 2018 / Published: 24 July 2018
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Abstract
The formation of nanoscale fibers from pH-sensitive polymers is a route which has been widely explored for targeted drug delivery. In particular, the Eudragit L100 and S100 families of polymers have received significant attention for this purpose. However, while in some cases it
[...] Read more.
The formation of nanoscale fibers from pH-sensitive polymers is a route which has been widely explored for targeted drug delivery. In particular, the Eudragit L100 and S100 families of polymers have received significant attention for this purpose. However, while in some cases it is shown that making drug-loaded Eudragit polymers effectively prevents drug release in low-pH media where the polymer is insoluble, this is not always the case, and other studies have reported significant amounts of drug release at acidic pHs. In this study, we sought to gain insight into the factors influencing the release of active ingredients from Eudragit S100 (ES100) fibers. A family of materials was prepared loaded with the model active ingredients (AIs) benzoic acid, 1-naphthoic acid, 1-naphthylamine, and 9-anthracene carboxylic acid. Analogous systems were prepared with an AI-loaded core and an ES100 sheath. The resultant fibers were smooth and cylindrical in the majority of cases, and X-ray diffraction and differential scanning calorimetry showed them to comprise amorphous solid dispersions. When AI release from the monolithic fibers was probed, it was found that there was significant release at pH 1 in all cases except with 9-anthracene carboxylic acid. Analysis of the results indicated that both the molecular weight of the AI and its acidity/basicity are important in controlling release, with lower molecular weight AIs and basic species released more quickly. The same release trends are seen with the core/shell fibers, but AI release at pH 1 is attenuated. The most significant change between the monolithic and core/shell systems was observed in the case of 1-naphthylamine. Mathematical equations were devised to connect molecular properties and AI release under acidic conditions. Full article
(This article belongs to the Special Issue Electrospun and Electrosprayed Formulations for Drug Delivery)
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