Bioavailability of phenolic compounds: a major challenge for drug development?

• Autor(a) principal: De Souza, Jacqueline Elis
• Data de Publicação: 2015
• Outros Autores: Casanova, Livia Marques, Costa, Sônia Soares
• Tipo de documento: Artigo
• Idioma: eng; por
• Título da fonte: Revista Fitos
• Texto Completo: https://revistafitos.far.fiocruz.br/index.php/revista-fitos/article/view/217
• topic: Substâncias fenólicas; Atividades biológicas; Metabolismo; Biodisponibilidade; Formulações; Pró-drogas; biological activities; metabolism; formulations; phytomedicines; pro-drugs.

Phenolic substances are an important class of secondary metabolites widely distributed in the plant kingdom. Several biological activities in vitro are assigned to this class of substances. However, some of these substances do not have the same profile of activity in in vivo assays. This fact could be partially explained by the low bioavailability of these substances. The main reasons for this low bioavailability may be low aqueous solubility, poor gastrointestinal stability and difficulty crossing membranes. The rapid and extensive metabolism by the intestinal flora and by some liver enzymes of phenolic substances after oral administration, may explain the poor bioavailability. In contrast, biotransformation can also lead to metabolites potentially more active than the original substances. Given the importance of the topic, this article aims to address the impacts of metabolism of phenolic substances on their pharmacological effects. Additionally, we show strategies to improve the bioefficacy of these substances, contributing to their use in the development of drugs of vegetal origin.