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).
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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.
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