Abstract

Tuberculosis (TB) is a dreadful bacterial disease, infecting millions of human and cattle every year worldwide. More than 50 years after its discovery, ethambutol continues to be an effective part of the World Health Organization’s recommended frontline chemotherapy against TB. However, the lengthy treatment regimens consisting of a cocktail of antibiotics affect patient compliance. There is an urgent need to improve the current therapy so as to reduce treatment duration and dosing frequency. In this study, we have designed a novel anti-TB multifunctional formulation by fabricating graphene oxide with iron oxide magnetite nanoparticles serving as a nano-carrier on to which ethambutol was successfully loaded. The designed nanoformulation was characterised using various analytical techniques. The release of ethambutol from anti-TB multifunctional nanoparticles formulation was found to be sustained over a significantly longer period of time in phosphate buffer saline solution at two physiological pH (7.4 and 4.8). Furthermore, the nano-formulation showed potent anti-tubercular activity while remaining non-toxic to the eukaryotic cells tested. The results of this in vitro evaluation of the newly designed nano-formulation endorse its further development in vivo.

Highlights

  • Tuberculosis (TB) is an infectious, bacterial disease caused by Mycobacterium tuberculosis (MTB)and it is a global health and economic concern, especially in the developing world [1,2]

  • Multifunctional nanoparticles that combine physico-chemical properties of different nanomaterials resulting in improved characteristics are highly sought after as drug delivery systems [6]

  • The FeNPs alone show five characteristic peaks because of (220), (311), (400), (422) and (511) planes at 2θ = 30.3◦, 35.7◦, 43.4◦, 53.6◦ and 57.3◦, respectively. These five peaks are an exact match to pure iron oxide magnetite nanoparticles showing a high purity of the designed FeNPs having cubic inverse spinel structure [28]

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Summary

Introduction

Tuberculosis (TB) is an infectious, bacterial disease caused by Mycobacterium tuberculosis (MTB)and it is a global health and economic concern, especially in the developing world [1,2]. Multifunctional nanoparticles that combine physico-chemical properties of different nanomaterials resulting in improved characteristics are highly sought after as drug delivery systems [6]. Graphene oxide (GO) is a promising material for biomedical applications, especially in drug delivery systems because of its two dimensional (2D) nanosize providing a large surface area with different functional groups, such as hydroxyl, carbonyl, epoxides, and unsaturated benzene rings [10,11]. These functional groups allow different drugs, hydrophilic and hydrophobic, to be loaded on GO. FeNPs have been widely applied in magnetic resonance imaging (MRI), hyperthermia, drug delivery, tissue repair, topical applications, bio-sensing, and bioanalysis [15,22,23,24,25,26]

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