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Nanostructured lipid system as carrier for benzofuroxanic derivative applicable in the study against Mycobacterium Tuberculosis

Grant number: 18/06098-6
Support type:Scholarships in Brazil - Scientific Initiation
Effective date (Start): June 01, 2018
Effective date (End): November 30, 2019
Field of knowledge:Biological Sciences - Microbiology - Applied Microbiology
Principal Investigator:Fernando Rogério Pavan
Grantee:Ana Carolina Lopes Silva
Home Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

Tuberculosis is the infectious disease that causes most deaths worldwide and Brazil is one of the 20 countries that register more incident cases. The emergence of multi-drug resistant strains has created a scenario with more complicated treatments and even incurable cases, and reports of resistance to new drugs that are still under clinical trials have already been observed. Benzofuroxane derivatives are an important class of heterocyclic compounds that have remarkable biological properties, including against Mycobacterium tuberculosis (MTB), due to their ability to generate reactive oxygen species. Nanostructured systems, such as microemulsions (MEs), can be used to encapsulate and deliver drugs, enhancing their oral bioavailability and promoting greater specificity for therapeutic targets. This work aims to characterize a ME containing a benzofuroxanic derivative - PJ10 (C18H18O3N4) by dynamic light scattering and zeta potential, as well as conducting the biological assays in vitro: minimum inhibitory concentration (MIC) against M. tuberculosis H37Rv, cytotoxicity (IC50) against cell lines J774A.1 (ATCC® TIB-67) and MRC-5 (ATCC® CCL-171) and the permeability through the monolayer of Caco-2 cells. It is hoped, therefore, to evaluate the properties of the nanostructured system in order to optimize the use of a benzofuroxanic derivative against MTB.