Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic resistant M. tuberculosis infections

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Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic resistant M. tuberculosis infections

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Publication Article, peer reviewed scientific
Title Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic resistant M. tuberculosis infections
Author Valetti, Sabrina ; Xia, Xin ; Costa-Gouveia, Joana ; Brodin, Priscille ; Bernet-Camard, Marie-Françoise ; Andersson, Margareta ; Feiler, Adam
Research Centre Biofilms - Research Center for Biointerfaces
Date 2017
English abstract
Aim: First extensive reformulation of clofazimine (CLZ) in nanoporous silica particles (NSPs) for tackling antibiotic-resistant tuberculosis (TB) infections. Materials & methods: Solid-state characterization of several CLZ-encapsulated NSP formulations was followed by in vitro drug solubility, Caco-2 intestinal cells drug permeability and TB antibacterial activity. Results: NSPs stabilize the amorphous state of CLZ (shelf stability >6 months) and dramatically increase the drug solubility in simulated gastric fluid (up to 20-fold) with different dissolution kinetics depending on the NSPs used. CLZ encapsulation in NSP substantially enhances the permeation through model intestinal cell layer, achieving effective antimicrobial concentrations in TB-infected macrophages. Conclusion: Promising results toward refurbishment of an approved marketed drug for a different indication suitable for oral anti-TB formulation.
DOI https://doi.org/10.2217/nnm-2016-0364 (link to publisher's fulltext.)
Link https://www.futuremedicine.com/doi/abs/10.2217/nnm... (external link to publication)
Publisher Future Medicine
Host/Issue Nanomedicine;8
Volume 12
ISSN 1743-5889
Language eng (iso)
Subject Caco-2 cells
HPLC
amorphous
clofazimine
drug carrier
intramacrophage in vitro assay
nanoporous silica particles
oral drug delivery
tuberculosis
Medicine
Research Subject Categories::PHARMACY
Handle http://hdl.handle.net/2043/24196 Permalink to this page
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