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Nano-Formulation of Ethambutol with Multifunctional Graphene Oxide and Magnetic Nanoparticles Retains Its Anti-Tubercular Activity with Prospects of Improving Chemotherapeutic Efficacy

Saifullah B 1 , Maitra A 2 , Chrzastek A 3 , Naeemullah B 4 , Fakurazi S 5 , Bhakta S 6 Show all authors , Hussein MZ 7

Affiliations 

  • 1 Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology (ISMB), Birkbeck, University of London, Malet Street, London WC1E 7HX, UK. [email protected]
  • 2 Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology (ISMB), Birkbeck, University of London, Malet Street, London WC1E 7HX, UK. [email protected]
  • 3 Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology (ISMB), Birkbeck, University of London, Malet Street, London WC1E 7HX, UK. [email protected]
  • 4 Department of Neurology (Ward No. 18), Jinnah Postgraduate Medical Center/Jinnah Sindh Medical, University Karachi, Karachi 75510, Pakistan. [email protected]
  • 5 Laboratory for Vaccine and Immunotherapeutics, Institute of Biosciences, Universiti Putra Malaysia (UPM), Serdang 43400, Selangor, Malaysia. [email protected]
  • 6 Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology (ISMB), Birkbeck, University of London, Malet Street, London WC1E 7HX, UK. [email protected]
  • 7 Material Synthesis and Characterization Laboratory, Institute of Advanced Technology (ITMA), Universiti Putra Malaysia (UPM), Serdang 43400, Selangor, Malaysia. [email protected]
Molecules, 2017 Oct 12;22(10).
PMID: 29023384 DOI: 10.3390/molecules22101697

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.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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