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Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic resistant M. tuberculosis infections
Malmö högskola, Faculty of Health and Society (HS), Department of Biomedical Science (BMV). Malmö högskola, Biofilms Research Center for Biointerfaces. Nanologica AB, 151 36, Södertälje, Sweden.ORCID iD: 0000-0002-2535-7108
Nanologica AB, SE-151 36 Södertälje, Sweden.
Univ. Lille, CNRS, INSERM, CHU Lille, Institut Pasteur deLille, U1019 - UMR 8204 - CIIL - Center for Infection & Immunity of Lille, F-59000 Lille, France.
Univ. Lille, CNRS, INSERM, CHU Lille, Institut Pasteur deLille, U1019 - UMR 8204 - CIIL - Center for Infection & Immunity of Lille, F-59000 Lille, France.
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2017 (English)In: Nanomedicine, ISSN 1743-5889, E-ISSN 1748-6963, Vol. 12, no 8Article in journal (Refereed)
Abstract [en]

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.

Place, publisher, year, edition, pages
Future Medicine , 2017. Vol. 12, no 8
Keywords [en]
Caco-2 cells, HPLC, amorphous, clofazimine, drug carrier, intramacrophage in vitro assay, nanoporous silica particles, oral drug delivery, tuberculosis
National Category
Medical and Health Sciences
Identifiers
URN: urn:nbn:se:mau:diva-4596DOI: 10.2217/nnm-2016-0364ISI: 000398957600003PubMedID: 28338408Scopus ID: 2-s2.0-85017365568Local ID: 24196OAI: oai:DiVA.org:mau-4596DiVA, id: diva2:1401428
Available from: 2020-02-28 Created: 2020-02-28 Last updated: 2024-06-17Bibliographically approved

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Publisher's full textPubMedScopushttps://www.futuremedicine.com/doi/abs/10.2217/nnm-2016-0364?rfr_dat=cr_pub%3Dpubmed&url_ver=Z39.88-2003&rfr_id=ori%3Arid%3Acrossref.org&journalCode=nnm

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Valetti, Sabrina

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