Efficacy of the treatment using a microemulsion loaded with epoxy-α-lapachone in combination with meglumine antimoniate against murine infection by Leishmania (Leishmania) amazonensis

Juliana Figueiredo Peixoto , Luiz Filipe Gonçalves-Oliveira , Franklin Souza-Silva , Luzia Monteiro de Castro Côrtes , Léa Cysne Finkelstein , Geovane Dias-Lopes , Beatriz Ferreira de Carvalho Patricio , Carolina Guimarães de Souza Lima , Helvécio Vinícius Antunes Rocha , Fernando de Carvalho da Silva , Vitor Francisco Ferreira , Bernardo Acácio Santini Pereira , Carlos Roberto Alves
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Abstract

Leishmaniasis is a disease caused by Leishmania spp., affecting millions of people around the world. For decades, its treatment has been based on pentavalent antimonials, which notoriously cause toxic side effects in patients. In this study, epoxy-α-lapachone incorporated into an oil-in-water-type microemulsion (ELAP-ME) and meglumine antimoniate (MA) were assayed in monotherapy and in combination (ELAP-ME/MA) in BALB/c mice infected with Leishmania (Leishmania) amazonensis. In general, there was a reduction in paw lesion size (up to 37% reduction) and decreases of parasite loads in the footpad (∼40%) and lymph nodes (∼31%) of animals treated with ELAP-ME/MA, when compared to the non-treated control groups. Analyses of serum biochemical parameters revealed that the ELAP-ME/MA showed lower renal and hepatic toxicity when compared to MA 2-doses/week monotherapy. These findings indicate that the ELAP-ME/MA combination may be a promising approach for the treatment of cutaneous leishmaniasis.

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使用含有环氧-α-拉帕醌的微乳剂与巨鲁明抗锑酸盐联合治疗小鼠亚马逊利什曼原虫感染的疗效
利什曼病是一种由利什曼原虫引起的疾病,影响着全世界数百万人。数十年来,治疗利什曼病一直使用五价抗锑剂,但这种药物会对患者产生毒副作用。在这项研究中,研究人员在感染了亚马逊利什曼原虫的 BALB/c 小鼠身上检测了掺入水包油型微乳剂(ELAP-ME)的环氧-α-拉帕醌和巨鲁明抗锑酸盐(MA)的单一疗法和组合疗法(ELAP-ME/MA)。总体而言,与未接受治疗的对照组相比,接受ELAP-ME/MA治疗的动物爪部病变面积缩小(最多缩小37%),足垫(∼40%)和淋巴结(∼31%)中的寄生虫数量减少。对血清生化指标的分析表明,ELAP-ME/MA与MA 2剂量/周单药治疗相比,肾毒性和肝毒性较低。这些研究结果表明,ELAP-ME/MA联合疗法可能是一种治疗皮肤利什曼病的有效方法。
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来源期刊
CiteScore
7.90
自引率
7.50%
发文量
31
审稿时长
48 days
期刊介绍: The International Journal for Parasitology – Drugs and Drug Resistance is one of a series of specialist, open access journals launched by the International Journal for Parasitology. It publishes the results of original research in the area of anti-parasite drug identification, development and evaluation, and parasite drug resistance. The journal also covers research into natural products as anti-parasitic agents, and bioactive parasite products. Studies can be aimed at unicellular or multicellular parasites of human or veterinary importance.
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