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The influence of recrystallized caffeine on water-swellable polymethacrylate mucoadhesive buccal films
College of Pharmacy, University of Texas at Austin.ORCID iD: 0000-0002-3190-2168
Department of Pharmacy and Pharmacology, University of Bath.
College of Pharmacy, University of Texas at Austin.
2013 (English)In: AAPS PharmSciTech, ISSN 1530-9932, E-ISSN 1530-9932, Vol. 14, no 2, 475-484 p.Article in journal (Refereed) Published
Abstract [en]

The aim of this work was to investigate the influence of particles on the properties of polymethacrylate films intended for buccal delivery. A solvent casting method was used with Eudragit RS and RL (ERS and ERL, respectively) as film-forming rate-controlling polymers, with caffeine as a water-soluble model drug. The physicochemical properties of the model films for a series of formulations with increasing concentrations of caffeine were determined in terms of morphology, mechanical and mucoadhesive properties, drug content uniformity, and drug release and associated kinetics. Typically regarded as non-mucoadhesive polymers, ERS and mainly ERL, were found to be good mucoadhesives, with ERL01 exhibiting a work of mucoadhesion (WoA) of 118.9 μJ, which was about five to six times higher than that observed for commonly used mucoadhesives such as Carbopol(®) 974P (C974P, 23.9 μJ) and polycarbophil (PCP, 17.4 μJ). The mucoadhesive force for ERL01 was found to be significantly lower yet comparable to C974P and PCP films (211.1 vs. 329.7 and 301.1 mN, respectively). Inspection of cross-sections of the films indicated that increasing the concentration of caffeine was correlated with the appearance of recrystallized agglomerates. In conclusion, caffeine agglomerates had detrimental effects in terms of mucoadhesion, mechanical properties, uniformity, and drug release at large particle sizes. ERL series of films exhibited very rapid release of caffeine while ERS series showed controlled release. Analysis of release profiles revealed that kinetics changed from a diffusion controlled to a first-order release mechanism.

Place, publisher, year, edition, pages
2013. Vol. 14, no 2, 475-484 p.
National Category
Pharmaceutical Sciences Other Health Sciences
Research subject
Health Science
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URN: urn:nbn:se:ltu:diva-64671DOI: 10.1208/s12249-012-9891-3PubMedID: 23456475Scopus ID: 2-s2.0-84879088162OAI: oai:DiVA.org:ltu-64671DiVA: diva2:1119614
Available from: 2017-07-04 Created: 2017-07-04 Last updated: 2017-11-29Bibliographically approved

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Morales, Javier O.

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