The Influence of Recrystallized Caffeine on Water-Swellable Polymethacrylate Mucoadhesive Buccal Films
Author
dc.contributor.author
Morales, Javier O.
Author
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Su, Rong
es_CL
Author
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McConville, Jason T.
es_CL
Admission date
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2014-01-29T12:44:23Z
Available date
dc.date.available
2014-01-29T12:44:23Z
Publication date
dc.date.issued
2013-06
Cita de ítem
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AAPS PharmSciTech, Vol. 14, No. 2, June 2013
en_US
Identifier
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DOI: 10.1208/s12249-012-9891-3
Identifier
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https://repositorio.uchile.cl/handle/2250/121784
General note
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Artículo de publicación ISI
en_US
Abstract
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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 watersoluble
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.