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3. Preformulation Studies of Novel Menthol Prodrugs with Antiparasitic Activity: Chemical Stability, In Silico, and In Vitro Permeability Assays.

Author

Clemente, Camila M., Onnainty, Renée, Usseglio, Nadina, Granero, Gladys E., and Ravetti, Soledad

Subjects
PRODRUGS, CHEMICAL stability, MENTHOL, PERMEABILITY, DRUG discovery, BIOLOGICAL membranes
Abstract

Based on the demonstrated and reported trypanocidal, leishmanicidal, and antiplasmodial activities of two menthol prodrugs, it was decided to proceed with preformulation studies, which are of key relevance in the drug discovery process. The aim of this study is to examine the stability and permeability of two new menthol prodrugs with antiparasitic activity. To determine the stability of menthol and its prodrugs, the corresponding studies were carried out in buffered solutions at pH values of 1.2, 5.8, and 7.4 at 37 °C. In silico permeability studies were performed using the free PerMM software and then in vitro permeability studies were performed using a biomimetic artificial membrane (BAM). Permeability studies conducted in silico predicted that both menthol and its prodrugs would pass through biological membranes via flip-flop movement. This prediction was subsequently confirmed by in vitro BAM permeability studies, where it was observed that the menthol prodrugs (1c and 1g) exhibited the highest Papp (apparent permeability) value compared to the parent compound. The study reveals that menthol prodrugs exhibit stability at a pH of 5.8 and possess sufficient in vitro permeability values as preformulation parameters. [ABSTRACT FROM AUTHOR]

Published
2023
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4. Standardization and organoleptic and physicochemical characterization of 15 argentinean propolis

Author

Lozina, Laura, Peichoto, Maria E., Acosta, Ofelia, and Granero, Gladys E.

Subjects
Farmacología, apis mellifera, caracterización, compuestos fenólicos, estandarización, flavonoides, propóleos, Medicamentos naturales, Compuestos fenólicos, Farmacia, characterization, flavonoids, phenolic compounds, propólis, standardization
Abstract

El propóleos es una mezcla de composición química compleja que posee propiedades biológicas de gran interés para fines terapéuticos. Existen distintos tipos de propóleos que difieren en su composición química de acuerdo a su origen botánico. En la actualidad se carece de un estándar de calidad de propóleos. Por esta razón, en este trabajo fueron determinados los caracteres organolépticos, propiedades físico- químicas y el contenido total de compuestos fenólicos y flavonoides de 15 muestras de propóleos recolectadas de diferentes regiones de Chaco, Corrientes, Santiago del Estero y Mendoza, para así brindar una estandarización que permita producir medicamentos de propóleos de seguridad y eficacia demostrable. Se encontró gran variación en las propiedades de los diferentes propóleos estudiados, incluso de aquellos provenientes de una misma región. Los propóleos difirieron principalmente en su contenido de compuestos fenólicos y flavonoides, siendo significativamente superiores en los propóleos originarios de Mendoza, donde la vegetación más abundante pertenece a Populus sp., Propolis is a mixture of complex chemical composition that possesses biological properties of great interest for therapeutic purposes. Different types of propolis exist, which differ in its chemical composition according to its botanical origin. At present, there is not a quality standard for propolis. For this reason, in this work the organoleptic characteristics, the physicochemical properties, the total content of phenolic compounds and the flavonoid composition of 15 samples of propolis collected from different regions of Chaco, Corrientes, Santiago del Estero, and Mendoza were determined, for providing an standardization that allows the production of effective and safe propolis products. It was found great variation in the properties of the different studied propolis, even of those from the same region. Principally, propolis differed in its phenolic and flavonoids content, being significantly higher in propolis from Mendoza, where the most abundant vegetation belongs to Populus sp., Colegio de Farmacéuticos de la Provincia de Buenos Aires

Published
2010

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