Formulación y evaluación biológica de nanomedicinas con extracto del cenizo Leucophyllum frutescens (BERL.) I.M. Johnston (Scrophulariaceae) contra Mycobacterium tuberculosis

Martínez Rivas, Claudia Janeth (2018) Formulación y evaluación biológica de nanomedicinas con extracto del cenizo Leucophyllum frutescens (BERL.) I.M. Johnston (Scrophulariaceae) contra Mycobacterium tuberculosis. Doctorado thesis, Universidad Autónoma de Nuevo León.

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Resumen

Tuberculosis is an emergency disease worldwide, the emergence of resistant strains to the treatment has produced the use of natural products as alternative. Studies have shown that Leucophyllum frutescens extracts present antimicrobial effect, but the disadvantage is that the extracts are recovered in a vehicle that contains organic solvents. The preparation of polymeric nanoparticles (NP) involves the elimination of the solvent in which the active is solubilized, which makes possible to use them as vehicles for the administration of the extracts. Therefore, the aim of this study was to design and develop formulations of NP with an extract of L. frutescens, and rifampicin (RIF), in order to evaluate the in vitro biological activity against M. tuberculosis. Firstly, the methanolic extract of leaves and roots of L. frutescens and its fractions were obtained. The anti-M. tuberculosis activity was determined, being the root extract (EMR) and its hexane fractions (FHR and RF1) the most actives with a MIC of 100, 40 and 40 ȝg/mL, respectively. RIF, EMH, FHR and RF1 were incorporated into NP by nanoprecipitation. NP of ≈180 nm with homogeneous size distribution were obtained. The NP were evaluated on M. tuberculosis, being the formulation of NP-PLGA-RIF (MIC=0.10 ȝg/mL) and NP-PLGA-RF1 (CMI=80 ȝg/mL) with better activity. Finally, the anti-M. tuberculosis activity of the combined form formulations was evaluated, the combination of RIF with NP-PLGA-RF1 produced better behavior, reducing the MIC of both without showing toxic effect. The studies carried out in this work showed the potential use of an NP formulation contains a vegetable fraction of L. frutescens in combination with RIF as an alternative against M. tuberculosis.

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