University of Hertfordshire

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Original languageEnglish
Number of pages11
Pages (from-to)164-174
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Journal publication date1 May 2017
Volume114
Early online date31 Jan 2017
DOIs
Publication statusPublished - 1 May 2017

Abstract

Film forming systems offer a number of advantages for topical and transdermal drug delivery, in particular enabling production of a supersaturated state which can greatly improve drug absorption and bioavailability. However the suitability of individual film forming polymers to stabilise the supersaturated state and optimise delivery of drugs is not well understood. This study reports the use of differential scanning calorimetry (DSC) to measure the solubility of methylphenidate both as the free base and as the hydrochloride salt in two polymethacrylate copolymers, Eudragit RS (EuRS) and Eudragit E (EuE) and relates this to the ability of films formed using these polymers to deliver methylphenidate across a model membrane. EuRS provided greater methylphenidate delivery when the drug was formulated as the free base in
comparison EuE because the lower solubility of the drug in EuRS provided a higher degree of drug saturation in the polymeric film. In contrast EuE provided greater delivery of methylphenidate hydrochloride as EuRS could not prevent its crystallisation from a supersaturated state. Methylphenidate flux across the membrane could be directly related to degree of saturation of the drug in the film formulation as estimated by the drug solubility in the individual polymers demonstrating the importance of drug solubility in the polymer included in film forming systems for topical/transdermal drug delivery. In addition DSC has been demonstrated to be a useful tool for determining the solubility of drugs in polymers used in film forming systems and the approaches outlined here are likely to be useful for predicting the suitability of polymers for particular drugs in film forming transdermal drug delivery systems.

Notes

© 2017 The Authors. Published by Elsevier B. V. This is an Open Access article distributed under the terms of the Creative Commons Attribution License CC-BY 4.0 ( https://creativecommons.org/licenses/by/4.0/ ) which permits unrestricted re-use, distribution, and reproduction in any medium, provided the original work is properly cited.

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