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Electrospinning optimization of Eudragit E PO with and without Chlorpheniramine Maleate using a Design of Experiment Approach

Abdelhakim, H; Coupe, A; Tuleu, C; Edirisinghe, M; Craig, D; (2019) Electrospinning optimization of Eudragit E PO with and without Chlorpheniramine Maleate using a Design of Experiment Approach. Molecular Pharmaceutics 10.1021/acs.molpharmaceut.9b00159. (In press). Green open access

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Abstract

Electrospinning is increasingly becoming a viable means of producing drug delivery vehicles for oral delivery, particularly as issues of manufacturing scalability are addressed. In this study, electrospinning is explored as a taste-masking manufacturing technology for bitter drugs. The taste-masking polymer Eudragit E PO (E-EPO) was electrospun, guided by a Quality by Design (QbD) approach. Using a Design of Experiment (DoE), factors influencing the production of smooth fibers were investigated. Polymer concentration, solvent composition, applied voltage, flow rate and gap distance were the parameters examined. Of these, polymer concentration was shown to be the only statistically significant factor within the ranges studied (p-value = 0.0042). As the concentration increased, smoother fibers were formed, coupled with an increase in fiber diameter. 35% w/v E-EPO was identified as the optimum concentration for smooth fiber production. The optimized processing conditions identified were a gap distance of 175 mm, applied voltage of between 15 kV and 20 kV and flow rate of 1 mL/hour. Using this knowledge, the production optimization of electrospun E-EPO with chlorpheniramine maleate (CPM), a bitter antihistamine drug, was explored. The addition of CPM in drug loads of 1:6 up to 1:10 CPM: EEPO yielded smooth fibers that were electrospun under similar conditions to placebo fibers. Solid state characterization showed CPM to be molecularly dispersed in E-EPO. An electronic tasting system, or E-tongue, indicated good taste-masking performance as compared to the equivalent physical mixtures. The study therefore describes a means of producing, optimizing and assessing the performance of electrospun taste-masked fibers as a novel approach to the formulation of CPM and potentially other bitter drug substances.

Type: Article
Title: Electrospinning optimization of Eudragit E PO with and without Chlorpheniramine Maleate using a Design of Experiment Approach
Open access status: An open access version is available from UCL Discovery
DOI: 10.1021/acs.molpharmaceut.9b00159
Publisher version: https://doi.org/10.1021/acs.molpharmaceut.9b00159
Language: English
Additional information: © 2019 American Chemical Society. ACS AuthorChoice. This is an open access article published under a Creative Commons Attribution (CC-BY) License, which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
Keywords: Electrospinning, taste-masking, E-tongue, Eudragit E PO, chlorpheniramine maleate, DoE
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics
UCL > Provost and Vice Provost Offices > UCL BEAMS
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Engineering Science
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Engineering Science > Dept of Mechanical Engineering
URI: https://discovery.ucl.ac.uk/id/eprint/10073184
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