Abstract
Las celdas de Franz son una de las herramientas para evaluar la permeación transepitelial de compuestos mediante la realización de ensayos in vitro, estos permiten inferir el comportamiento de seguridad de un compuesto en la piel. El objetivo de esta investigación fue determinar el comportamiento de permeación del ácido benzoico a partir de complejos con polielectrolitos () en comparación con el ácido benzoico sin complejar, para inferir su comportamiento de seguridad. En una primera fase, se establecieron las condiciones de almacenamiento de la piel comparando los parámetros de difusión (flujo y constante de permeación) y pérdida de agua transepitelial, empleando piel de orejas de cerdos recién sacrificados, almacenadas en NaCl 1M a -2°C por 3 días; se trabajó bajo condiciones de dosis infinitas. Posteriormente, se realizó el ensayo de permeación de dos complejos entre ácido benzoico y Eudragit E, en comparación con el ácido benzoico, bajo condiciones de dosis finitas. La cuantificación del ácido benzoico fue realizada con un método analítico validado por HPLC-DAD. Los resultados evidenciaron que las muestras biológicas pueden almacenarse durante 72 h en las condiciones descritas. El comportamiento de permeación del ácido benzoico complejado respecto al ácido benzoico libre demostró tener un mejor perfil de seguridad, puesto que hubo una menor permeación para el primer caso. Estos resultados demuestran que la complejación del ácido benzoico podría disminuir las reacciones de sensibilidad que normalmente este presenta, basándose en la disminución de su permeación.
Highlights
Preservatives are widely used and necessary in all products with risk of deterioration because by inhibiting the growth of bacteria and fungi they prevent microbiological contamination of the product, protecting the consumer from possible infection [1]
In vitro tests conducted in Franz cells are considered as one of the main tools to evaluate transepithelial permeation, which consist of two compartments, one donor and another recipient where it is sampled periodically to evaluate the amount of compound that has penetrated through tissue over time [6]
Permeation tests were performed with benzoic acid and with the complexes(EuB(7E5CuBl2755,CaEnlu2d5B,1E00u)B100 )(figure 2) generated by the ionic interactions of the molecules involved, where Eu corresponds to the Eudragit E100 polyelectrolyte, B to the benzoate ion and Cl to the chloride ion that act as counterions, the subscripts indicate the percentage at which each counterion is neutralizing the polymer; these complexes have shown in previous studies carried out within the research group, that their antimicrobial activity is maintained [4, 6]
Summary
Preservatives are widely used and necessary in all products with risk of deterioration because by inhibiting the growth of bacteria and fungi they prevent microbiological contamination of the product, protecting the consumer from possible infection [1]. Despite being considered a harmless substance, its topical application can generate hives, erythema, and stinging, probably by induction in the skin of large amounts of prostaglandin D2 [3] In this sense, possible strategies that reduce the allergic reactions normally presented by this preservative have been evaluated, and the formation of complexes with polyelectrolytes is an important alternative because they modify its physicochemical properties, functionality and could even improve its safety [4]. In vitro tests conducted in Franz cells are considered as one of the main tools to evaluate transepithelial permeation, which consist of two compartments, one donor and another recipient where it is sampled periodically to evaluate the amount of compound that has penetrated through tissue over time [6]. This work is intended to assess whether there is a difference in the permeation behavior of complexes containing benzoic acid against the uncomplexed compound, from which it could be inferred if there is a difference in their biological safety
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