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

Jesús Israel Rodríguez, Rosa Isela Sánchez, Marianela Garza, María Argelia Nakagoshi, Juan Manuel Solis, Katiushka Arévalo, Emmanuel Garza


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.


Biofilms, Pilocarpine, Hyposalivation, Chitosan.


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