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Fluorescence imaging of antibiotic clofazimine encapsulated within mesoporous silica particle carriers: relevance to drug delivery and the effect on its release kinetics
Departamento de Química Física, Facultad de Ciencias del Medio Ambiente y Bioquímica and INAMOL, Universidad de Castilla-La Mancha, Avenida Carlos III, S/N, 45071 Toledo, Spain..
Malmö University, Faculty of Health and Society (HS), Department of Biomedical Science (BMV). Malmö University, Biofilms Research Center for Biointerfaces. Nanologica AB, Södertälje, SE-151 36, Sweden.ORCID iD: 0000-0002-2535-7108
Departamento de Química Física, Facultad de Ciencias Del Medio Ambiente y Bioquímica, INAMOL, Universidad de Castilla-La Mancha, Avenida Carlos III, S/N, Toledo, 45071, Spain.
Nanologica AB, Södertälje, SE-151 36, Sweden; Surface and Corrosion Science, KTH Royal Institute of Technology, Stockholm, SE-100 44, Sweden.
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2018 (English)In: Physical Chemistry, Chemical Physics - PCCP, ISSN 1463-9076, E-ISSN 1463-9084, Vol. 20, no 17, p. 11899-11911Article in journal (Refereed)
Abstract [en]

We report on the encapsulation of the antibiotic clofazimine (CLZ) within the pores of mesoporous silica particles having hydrophilic (CBET value of 137) and more hydrophobic (CBET value of 94 after calcination at 600 °C) surfaces. We studied the effect of pH on the released amount of CLZ in aqueous solutions and observed a maximum at pH 4.1 in correlation with the solubility of the drug. Less release of the drug was observed from the more hydrophobic particles which was attributed to a difference in the affinity of the drug to the carrier particles. Fluorescence lifetime imaging microscopy, emission spectra, and fluorescence lifetimes of single drug loaded particles provided detailed understanding and new knowledge of the physical form of the encapsulated drug and the distribution within the particles. The distribution of CLZ within the particles was independent of the surface chemistry of the particles. The confirmation of CLZ molecules as monomers or aggregates was revealed by controlled removal of the drug with solvent. Additionally, the observed optical "halo effect" in the fluorescent images was interpreted in terms of specific quenching of high concentration of molecules. The emission lifetime experiments suggest stronger interaction of CLZ with the more hydrophobic particles, which is relevant to its release. The results reported in this work demonstrate that tuning the hydrophilicity/hydrophobicity of mesoporous silica particles can be used as a tool to control the release without impacting their loading ability.

Place, publisher, year, edition, pages
Royal Society of Chemistry, 2018. Vol. 20, no 17, p. 11899-11911
Keywords [en]
drug delivery, mesoporous silica particle, clofazimine, fluorescence imaging, Clofazimine, Drug Carriers, Drug Delivery Systems, Drug Liberation, Fluorescence, Kinetics, Silicon Dioxide
National Category
Engineering and Technology
Identifiers
URN: urn:nbn:se:mau:diva-5574DOI: 10.1039/c7cp08328aISI: 000431824000044PubMedID: 29666860Scopus ID: 2-s2.0-85046692379Local ID: 26776OAI: oai:DiVA.org:mau-5574DiVA, id: diva2:1402436
Available from: 2020-02-28 Created: 2020-02-28 Last updated: 2024-06-17Bibliographically approved

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Publisher's full textPubMedScopushttp://pubs.rsc.org/en/Content/ArticleLanding/2018/CP/C7CP08328A#!divAbstract

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Valetti, Sabrina

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