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Transport of Lipophilic Anti‐Tuberculosis Drug Benzothiazone‐043 in Ca3(PO4)2 Nanocontainers
ChemNanoMat ( IF 3.8 ) Pub Date : 2020-10-28 , DOI: 10.1002/cnma.202000421
David Rudolph 1 , Natalja Redinger 2 , Ulrich E. Schaible 2 , Claus Feldmann 1
Affiliation  

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@Ca3(PO4)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 Ca2+, followed by the formation of an inorganic Ca3(PO4)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@Ca3(PO4)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@Ca3(PO4)2 nanocontainers.

中文翻译:

亲脂性抗结核药物Benzothiazone-043在Ca3(PO4)2纳米容器中的运输

1,3-苯并噻嗪-4-043(BTZ043)是一种新型的抗结核菌药物,具有高度疏水性,适用于结核病(TB)治疗。为了通过改善给药和分枝杆菌感染部位的给药来提高局部药物浓度,我们建议通过微乳液方法制备的BTZ043 / Toc @ Ca(ds)2 @Ca 3(PO 42纳米容器用于给药(Toc :生育酚; ds:十二烷基硫酸盐)。根据我们的概念,微乳液本身的表面活性剂可通过与Ca 2+相互作用来稳定液滴相,然后形成无机Ca 3(PO 42一锅反应中的球体壁。生育酚(维生素E)用作微乳液的生物相容性液滴相,以溶解高度亲脂的BTZ043。根据电子显微镜和电子光谱法,所得的BTZ043 / Toc @ Ca(ds)2 @Ca 3(PO 42纳米容器具有28±8nm的外径和4±1nm的球壁。直径18±7 nm的内腔装有浓度为30.5μg/ mL的BTZ043。对结核分枝杆菌感染的小鼠骨髓衍生的巨噬细胞进行的首次体外测试显示,BTZ043 / Toc @ Ca(ds)2 @Ca 3(PO 42个纳米容器。
更新日期:2020-10-28
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