Artigo Produção Nacional Revisado por pares

Design and characterization of a tuberculostatic hybrid based on interaction of ethambutol with a raw palygorskite

2019; Elsevier BV; Volume: 181; Linguagem: Inglês

10.1016/j.clay.2019.105213

ISSN

1872-9053

Autores

Lyghia Maria Araújo Meirelles, Esperanza Carazo, Ana Borrego‐Sánchez, Raquel de Melo Barbosa, Túlio Flávio Accioly de Lima e Moura, Carola Aguzzi, C. Ignacio Sainz‐Díaz, César Viseras, Fernanda Nervo Raffin,

Tópico(s)

Layered Double Hydroxides Synthesis and Applications

Resumo

Treatment of tuberculosis (TB) based on ethambutol (ETB) in combination with other tuberculostatic agents has technological challenges due to physical instability and drug incompatibilities. Alternative formulations using clay minerals have been successfully designed. In this study, a hybrid (ETB/Pal) based on ETB and a Brazilian palygorskite (Pal) was prepared and characterized by adsorption study and diverse solid-state techniques. In addition, hygroscopicity study and in vitro release assays of ETB from the nanohybrid were performed and supported by molecular modelling study. The adsorption of ETB on Pal occurred as a spontaneous process, with around 15.9% (w/w) retained in the hybrid. Characterization of the ETB/Pal showed a change in the surface charge of Pal attributed to an electrostatic interaction between ionized amine groups from ETB and the electronegative surface of the silicate. Furthermore, molecular modelling confirmed the obtention of a nanohybrid formed mainly by hydrogen bonds between surface O atoms of Pal and hydrophilic groups of ETB. Microanalysis showed the presence and homogeneous distribution of the drug on the nanohybrid. Elucidation of the interactions between ETB and this raw clay reinforces its viability as a novel carrier to reduce the humidity adsorption by the anti-TB drugs mixture, increasing the physical stability of the formulation.

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