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Nano-Based Drug Delivery Systems of Potent MmpL3 Inhibitors for Tuberculosis Treatment
Tuberculosis remains one of the world’s deadliest infectious diseases, accounting for nearly 1.3 million deaths every year. Tuberculosis treatment is challenging because of the toxicity, decreased bioavailability at the target site of the conventional drugs and, most importantly, low adherence of pa...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8955761/ https://www.ncbi.nlm.nih.gov/pubmed/35335983 http://dx.doi.org/10.3390/pharmaceutics14030610 |
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author | Hanieh, Patrizia Nadia Consalvi, Sara Forte, Jacopo Cabiddu, Gianluigi De Logu, Alessandro Poce, Giovanna Rinaldi, Federica Biava, Mariangela Carafa, Maria Marianecci, Carlotta |
author_facet | Hanieh, Patrizia Nadia Consalvi, Sara Forte, Jacopo Cabiddu, Gianluigi De Logu, Alessandro Poce, Giovanna Rinaldi, Federica Biava, Mariangela Carafa, Maria Marianecci, Carlotta |
author_sort | Hanieh, Patrizia Nadia |
collection | PubMed |
description | Tuberculosis remains one of the world’s deadliest infectious diseases, accounting for nearly 1.3 million deaths every year. Tuberculosis treatment is challenging because of the toxicity, decreased bioavailability at the target site of the conventional drugs and, most importantly, low adherence of patients; this leads to drug resistance. Here, we describe the development of suitable nanocarriers with specific physicochemical properties to efficiently deliver two potent antimycobacterial compounds. We prepared nanoemulsions and niosomes formulations and loaded them with two different MmpL3 inhibitors previously identified (NEs + BM635 and NIs + BM859). NEs + BM635 and NIs + BM859 were deeply characterized for their physicochemical properties and anti-mycobacterial activity. NEs + BM635 and NIs + BM859 showed good hydrodynamic diameter, ζ-Potential, PDI, drug-entrapment efficiency, polarity, and microviscosity and stability. Even though both formulations proved to perform well, only NIs + BM859 showed potent antimycobacterial activity against M. tuberculosis (MIC = 0.6 µM) compared to that of the free compound. This is most probably caused by the fact that BM635, being highly hydrophobic, encounters maximum hindrance in diffusion, whereas BM859, characterized by high solubility in aqueous medium (152 µM), diffuses more easily. The niosomal formulation described in this work may be a useful therapeutic tool for tuberculosis treatment, and further studies will follow to characterize the in vivo behavior of the formulation. |
format | Online Article Text |
id | pubmed-8955761 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-89557612022-03-26 Nano-Based Drug Delivery Systems of Potent MmpL3 Inhibitors for Tuberculosis Treatment Hanieh, Patrizia Nadia Consalvi, Sara Forte, Jacopo Cabiddu, Gianluigi De Logu, Alessandro Poce, Giovanna Rinaldi, Federica Biava, Mariangela Carafa, Maria Marianecci, Carlotta Pharmaceutics Article Tuberculosis remains one of the world’s deadliest infectious diseases, accounting for nearly 1.3 million deaths every year. Tuberculosis treatment is challenging because of the toxicity, decreased bioavailability at the target site of the conventional drugs and, most importantly, low adherence of patients; this leads to drug resistance. Here, we describe the development of suitable nanocarriers with specific physicochemical properties to efficiently deliver two potent antimycobacterial compounds. We prepared nanoemulsions and niosomes formulations and loaded them with two different MmpL3 inhibitors previously identified (NEs + BM635 and NIs + BM859). NEs + BM635 and NIs + BM859 were deeply characterized for their physicochemical properties and anti-mycobacterial activity. NEs + BM635 and NIs + BM859 showed good hydrodynamic diameter, ζ-Potential, PDI, drug-entrapment efficiency, polarity, and microviscosity and stability. Even though both formulations proved to perform well, only NIs + BM859 showed potent antimycobacterial activity against M. tuberculosis (MIC = 0.6 µM) compared to that of the free compound. This is most probably caused by the fact that BM635, being highly hydrophobic, encounters maximum hindrance in diffusion, whereas BM859, characterized by high solubility in aqueous medium (152 µM), diffuses more easily. The niosomal formulation described in this work may be a useful therapeutic tool for tuberculosis treatment, and further studies will follow to characterize the in vivo behavior of the formulation. MDPI 2022-03-10 /pmc/articles/PMC8955761/ /pubmed/35335983 http://dx.doi.org/10.3390/pharmaceutics14030610 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Hanieh, Patrizia Nadia Consalvi, Sara Forte, Jacopo Cabiddu, Gianluigi De Logu, Alessandro Poce, Giovanna Rinaldi, Federica Biava, Mariangela Carafa, Maria Marianecci, Carlotta Nano-Based Drug Delivery Systems of Potent MmpL3 Inhibitors for Tuberculosis Treatment |
title | Nano-Based Drug Delivery Systems of Potent MmpL3 Inhibitors for Tuberculosis Treatment |
title_full | Nano-Based Drug Delivery Systems of Potent MmpL3 Inhibitors for Tuberculosis Treatment |
title_fullStr | Nano-Based Drug Delivery Systems of Potent MmpL3 Inhibitors for Tuberculosis Treatment |
title_full_unstemmed | Nano-Based Drug Delivery Systems of Potent MmpL3 Inhibitors for Tuberculosis Treatment |
title_short | Nano-Based Drug Delivery Systems of Potent MmpL3 Inhibitors for Tuberculosis Treatment |
title_sort | nano-based drug delivery systems of potent mmpl3 inhibitors for tuberculosis treatment |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8955761/ https://www.ncbi.nlm.nih.gov/pubmed/35335983 http://dx.doi.org/10.3390/pharmaceutics14030610 |
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