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Molecules 2016, 21(6), 702; doi:10.3390/molecules21060702

Inhalable Antitubercular Therapy Mediated by Locust Bean Gum Microparticles

1
Center for Biomedical Research (CBMR), Faculty of Sciences and Technology, University of Algarve, 8005-139 Faro, Portugal
2
Centre for Marine Sciences (CCMar), University of Algarve, 8005-139 Faro, Portugal
3
Centro de Química Estrutural (CQE), Instituto Superior Técnico, University of Lisbon, 1049-001 Lisbon, Portugal
4
Algarve Chemistry Research Center (CIQA) and Department of Chemistry and Pharmacy, Faculty of Sciences and Technology, University of Algarve, 8005-139 Faro, Portugal
*
Author to whom correspondence should be addressed.
Academic Editor: Peter J. Rutledge
Received: 13 February 2016 / Revised: 14 May 2016 / Accepted: 19 May 2016 / Published: 28 May 2016
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Abstract

Tuberculosis remains a major global health problem and alternative therapeutic approaches are needed. Considering the high prevalence of lung tuberculosis (80% of cases), the pulmonary delivery of antitubercular drugs in a carrier system capable of reaching the alveoli, being recognised and phagocytosed by alveolar macrophages (mycobacterium hosts), would be a significant improvement to current oral drug regimens. Locust bean gum (LBG) is a polysaccharide composed of galactose and mannose residues, which may favour specific recognition by macrophages and potentiate phagocytosis. LBG microparticles produced by spray-drying are reported herein for the first time, incorporating either isoniazid or rifabutin, first-line antitubercular drugs (association efficiencies >82%). Microparticles have adequate theoretical properties for deep lung delivery (aerodynamic diameters between 1.15 and 1.67 μm). The cytotoxic evaluation in lung epithelial cells (A549 cells) and macrophages (THP-1 cells) revealed a toxic effect from rifabutin-loaded microparticles at the highest concentrations, but we may consider that these were very high comparing with in vivo conditions. LBG microparticles further evidenced strong ability to be captured by macrophages (percentage of phagocytosis >94%). Overall, the obtained data indicated the potential of the proposed system for tuberculosis therapy. View Full-Text
Keywords: alveolar macrophages; antitubercular drugs; inhalable therapy; locust bean gum; microparticles; spray-drying; tuberculosis therapy alveolar macrophages; antitubercular drugs; inhalable therapy; locust bean gum; microparticles; spray-drying; tuberculosis therapy
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Alves, A.D.; Cavaco, J.S.; Guerreiro, F.; Lourenço, J.P.; Rosa da Costa, A.M.; Grenha, A. Inhalable Antitubercular Therapy Mediated by Locust Bean Gum Microparticles. Molecules 2016, 21, 702.

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