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首页> 外文期刊>PLOS Neglected Tropical Diseases >In Vitro and In Vivo Trypanocidal Activity of H2bdtc-Loaded Solid Lipid Nanoparticles
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In Vitro and In Vivo Trypanocidal Activity of H2bdtc-Loaded Solid Lipid Nanoparticles

机译：H2bdtc负载固体脂质纳米粒子的体外和体内锥虫杀虫活性。

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摘要

The parasite Trypanosoma cruzi causes Chagas disease, which remains a serious public health concern and continues to victimize thousands of people, primarily in the poorest regions of Latin America. In the search for new therapeutic drugs against T. cruzi, here we have evaluated both the in vitro and the in vivo activity of 5-hydroxy-3-methyl-5-phenyl-pyrazoline-1-(S-benzyl dithiocarbazate) (H2bdtc) as a free compound or encapsulated into solid lipid nanoparticles (SLN); we compared the results with those achieved by using the currently employed drug, benznidazole. H2bdtc encapsulated into solid lipid nanoparticles (a) effectively reduced parasitemia in mice at concentrations 100 times lower than that normally employed for benznidazole (clinically applied at a concentration of 400 μmol kg?1 day?1); (b) diminished inflammation and lesions of the liver and heart; and (c) resulted in 100% survival of mice infected with T. cruzi. Therefore, H2bdtc is a potent trypanocidal agent.
机译：克氏锥虫寄生虫引起南美锥虫病，这仍然是严重的公共卫生问题，并继续使成千上万人受害，主要是在拉丁美洲最贫穷的地区。在寻找针对克氏锥虫的新治疗药物时，我们在此评估了5-羟基-3-甲基-5-苯基-5-吡唑啉-1-（S-苄基二硫代氨基甲酸酯）（H2bdtc）的体外和体内活性）作为游离化合物或封装在固体脂质纳米颗粒（SLN）中;我们将结果与使用当前使用的药物苯硝唑获得的结果进行了比较。封装在固体脂质纳米颗粒中的H2bdtc（a）有效降低小鼠体内的寄生虫病，其浓度比苯硝唑通常使用的浓度低100倍（临床应用浓度为400μmolkg？1天？1）; （b）减轻了肝脏和心脏的炎症和损害; （c）导致感染了克氏锥虫的小鼠存活率达到100％。因此，H2bdtc是有效的锥虫杀虫剂。

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