Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic resistant M. tuberculosis infectionsShow others and affiliations
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
2020-02-282020-02-282024-06-17Bibliographically approved