纳米体系中环氧化拉帕醌：用于利什曼病的原型药物，在二项式 BALB/c-利什曼原虫（利什曼原虫）亚马逊亚种中进行评估。

Epoxy-a-lapachone in nanosystem: a prototype drug for leishmaniasis assessed in the binomial BALB/c - Leishmania (Leishmania) amazonensis.

机构信息

Universidade Católica de Petrópolis, Petrópolis, RJ, Brasil.

Fundação Oswaldo Cruz-Fiocruz, Instituto Oswaldo Cruz, Laboratório de Biologia Molecular e Doenças Endêmicas, Rio de Janeiro, RJ, Brasil.

出版信息

Mem Inst Oswaldo Cruz. 2024 Oct 28;119:e240115. doi: 10.1590/0074-02760240115. eCollection 2024.

DOI:10.1590/0074-02760240115

PMID:39476028

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11520661/

Abstract

This perspective presents and supports arguments for a new formulation of epoxy-α-lapachone loaded microemulsion (ELAP-ME), a nanosystem, as a prototype drug for the treatment of leishmaniasis. The benefits of ELAP as a multitarget compound, with properties that affect key physiological pathways of Leishmania spp. are discussed. ELAP-ME demonstrated efficacy in murine infection models, particularly with the binomial BALB/c-Leishmania (Leishmania) amazonensis. Furthermore, it is proposed that the technological maturity of ELAP-ME be classified as Technology Readiness Level 4 (TLR 4) within the context of innovative drugs for American Cutaneous Leishmaniasis (ACL).

摘要

本文提出并支持了一种新的环氧化-α-拉帕醌负载型微乳液（ELAP-ME）的制剂形式，即纳米系统，作为治疗利什曼病的原型药物。本文讨论了 ELAP 作为一种多靶点化合物的优势，其具有影响利什曼原虫关键生理途径的特性。ELAP-ME 在小鼠感染模型中表现出疗效，特别是在二项式 BALB/c-利什曼原虫（利什曼原虫）亚马逊亚种中。此外，本文还提出，ELAP-ME 的技术成熟度应在治疗美洲皮肤利什曼病（ACL）的创新药物的背景下被归类为技术就绪水平 4（TLR 4）。