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Transport of Lipophilic Anti‐Tuberculosis Drug Benzothiazone‐043 in Ca 3 (PO 4 ) 2 Nanocontainers
Author(s) -
Rudolph David,
Redinger Natalja,
Schaible Ulrich E.,
Feldmann Claus
Publication year - 2021
Publication title -
chemnanomat
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.947
H-Index - 32
ISSN - 2199-692X
DOI - 10.1002/cnma.202000421
Subject(s) - microemulsion , chemistry , pulmonary surfactant , nuclear chemistry , drug delivery , zeta potential , scanning electron microscope , mycobacterium tuberculosis , chromatography , materials science , nanoparticle , nanotechnology , organic chemistry , tuberculosis , biochemistry , medicine , pathology , composite material
1,3‐Benzothiazin‐4‐one‐043 (BTZ043) is a novel anti‐mycobacterial agent for tuberculosis (TB) therapy with highly hydrophobic properties. In order to enhance local drug concentrations by improved administration and delivery to the site of the mycobacterial infection, we suggest BTZ043/Toc@Ca(ds) 2 @Ca 3 (PO 4 ) 2 nanocontainers made via a microemulsion approach for drug delivery (Toc: tocopherol; ds: dodecylsulfate). Based on our concept, the surfactant of the microemulsion itself is used to stabilize the droplet phase by interaction with Ca 2+ , followed by the formation of an inorganic Ca 3 (PO 4 ) 2 sphere wall in one‐pot reaction. Tocopherol (vitamin E) was used as biocompatible droplet phase of the microemulsion to dissolve the highly lipophilic BTZ043. According to electron microscopy and electron spectroscopy, the resulting BTZ043/Toc@Ca(ds) 2 @Ca 3 (PO 4 ) 2 nanocontainers exhibit an outer diameter of 28±8 nm and a sphere wall of 4±1 nm. The inner cavity, 18±7 nm in diameter, is loaded with BTZ043 with a concentration of 30.5 μg/mL. First in vitro tests with murine bone marrow derived macrophages infected with Mycobacterium tuberculosis show promising antibiotic activity of the BTZ043/Toc@Ca(ds) 2 @Ca 3 (PO 4 ) 2 nanocontainers.