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Pharmaceutics 2018, 10(3), 103; https://doi.org/10.3390/pharmaceutics10030103

The Effect of Molecular Properties on Active Ingredient Release from Electrospun Eudragit Fibers

UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK
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Received: 16 March 2018 / Revised: 11 May 2018 / Accepted: 16 May 2018 / Published: 24 July 2018
(This article belongs to the Special Issue Electrospun and Electrosprayed Formulations for Drug Delivery)
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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 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. View Full-Text
Keywords: electrospinning; Eudragit; nanofibers; drug release electrospinning; Eudragit; nanofibers; drug release
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Burgess, K.; Li, H.; Abo-zeid, Y.; Fatimah; Williams, G.R. The Effect of Molecular Properties on Active Ingredient Release from Electrospun Eudragit Fibers. Pharmaceutics 2018, 10, 103.

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