Physico-chemical and antimicrobial evaluation of chitosan and hydroxypropyl methylcellulose biofilms for prolonged release of pilocarpine

Introduction: The local use of prolonged drug delivery in the oral cavity provides many advantages, increasing the pharmacologic action in the local desirable site, the reduction of the usual dose and reduced adverse effects. Pilocarpine is a cholinergic drug approved by the FDA for the treatment of...

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Veröffentlicht in:Journal of oral research 2015, Vol.4 (1), p.25-31
Hauptverfasser: Rodríguez, Jesús Israel, Nakagoshi, María Argelia, Solis, Juan Manuel, Garza, Emmanuel, Garza, Marianela, Sánchez, Rosa Isela, Arévalo, Katiushka
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Sprache:eng
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Zusammenfassung:Introduction: The local use of prolonged drug delivery in the oral cavity provides many advantages, increasing the pharmacologic action in the local desirable site, the reduction of the usual dose and reduced adverse effects. Pilocarpine is a cholinergic drug approved by the FDA for the treatment of glandular hypofunction, however the diversity of the adverse effects limit their use.Objective: The principal aim of this study is analyze the physical and chemical properties of biofilms including the pH, thickness, solubility, consistency and the ability to release for prolonged time pilocarpine, and also assess the antimicrobial activity in two opportunistic pathogens in hyposialia (Streptococcus mutans and Candida albicans). Methods: Chitosan and HPMC (Methocel K4MCR) biofilms were prepared in 1% acetic acid, added with pilocarpine by magnetic stirring, assessing the pH, thickness and time of solubility in artificial saliva, as well as the uniformity of distribution and kinetics drug release per cm2 by spectrophotometry (OD = 420nm). The antimicrobial activity was test by disk diffusion against St. mutans ATCC 700610 and C. albicans ATCC 90029 at concentrations of hyposalivation (1.44 x 1.2 x 106 CFU and 103 CFU, respectively).Results: All biofilms, except for Hydroxypropylmethylcellulose and Hydroxypropylmethylcellulose / Pilocarpine formulation were found to have the optimal physicochemical properties for handling, maintaining a uniform distribution of the drug in 76% per cm2 with extended release during 4 hours, but showing negative antimicrobial activity in concentrations of hyposalivation.Conclusion: The films had optimum handling properties, and constant release of the drug, however, antimicrobial activity was not found. Introducción: El uso local de administración prolongada de fármacos en la cavidad oral proporciona múltiples ventajas, aumentando la acción farmacológica en el sitio local deseable, reducción de la dosis usual y disminución de los efectos adversos. La pilocarpina es una droga colinérgica aprobada por la FDA para el tratamiento de la hipofunción glandular, sin embargo la amplitud de sus efectos adversos limitan su uso.Objetivo: Con el objetivo de analizar las propiedades físico-químicas de las biopelículas se evaluó el pH, grosor, solubilidad, uniformidad y la capacidad de liberar prolongadamente pilocarpina, así como su actividad antimicrobiana ante los dos microorganismos patógenos oportunistas en la hiposialia (Streptococcus mutans
ISSN:0719-2460
0719-2479
0719-2479