青蒿素给药的新前景:在实验性内脏利什曼病中的生产和疗效。

IF 4.9 4区 医学 Q1 PARASITOLOGY Pathogens and Global Health Pub Date : 2024-02-01 Epub Date: 2023-05-15 DOI:10.1080/20477724.2023.2212347
Maryam Akbari, Hossein Heli, Ahmad Oryan, Gholamreza Hatam
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引用次数: 0

摘要

由婴儿利什曼原虫感染引起的内脏型利什曼病(VL)是一种被忽视的热带疾病。可供选择的治疗方案十分有限。青蒿素是一种高效的抗利什曼病药,但生物可用性较差,在治疗 VL 时需要高剂量的重复治疗。固体脂质纳米颗粒(SLNs)可提供靶向给药,提高生物利用率,降低传统治疗策略的毒性。制备出的球形青蒿素负载 SLNs 的颗粒直径为 222.0 ± 14.0 nm。SLNs对寄生虫没有特别的毒性作用,而本地青蒿素在250微克/毫升的浓度下,对原虫的存活率有31%的显著毒性作用。在本研究中,青蒿素载体 SLNs 在实验性 VL 中的疗效得到了证实,实验对象是受婴儿疟原虫感染的 BALB/c 小鼠。与游离青蒿素相比,10 毫克/千克和 20 毫克/千克剂量的青蒿素负载 SLNs 显示出更高水平的抗利什曼病疗效。与游离青蒿素相比,20 毫克/千克剂量的青蒿素负载 SLNs 能明显减轻肝脏(84.7 ± 4.9%)和脾脏(85.0 ± 3.1%)中的寄生虫负担,并减轻肝脾肿大。因此,本研究证实了青蒿素负载SLNs的疗效优于游离青蒿素,可作为治疗利什曼病的一种新疗法。
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A novel outlook in the delivery of artemisinin: production and efficacy in experimental visceral leishmaniasis.

The visceral form of leishmaniasis (VL), due to infection by Leishmania infantum, is a neglected tropical disease. The accessible therapeutic options are limited. Artemisinin is an efficient antileishmanial product with poor biological availability that requires high repetition of therapeutic doses in VL. Solid lipid nanoparticles (SLNs) provide targeted delivery, increase bioavailability and reduce toxicity of the traditional therapeutic strategy. The spherical shape artemisinin-loaded SLNs were prepared in a particle diameter of 222.0 ± 14.0 nm. The SLNs showed no particular toxic effect on the parasites, whereas the native artemisinin demonstrated a significant toxicity rate of 31% in viability of the promastigotes at the 250 µg/ml concentration. The therapeutic efficacy of the artemisinin-loaded SLNs was demonstrated in the experimental VL, using the L. infantum-infected BALB/c mice, in the present study. The 10 and 20 mg/kg doses of artemisinin-loaded SLNs showed higher level of antileishmanial efficacy compared with the free artemisinin. There was a significant diminishing of the parasite burden in liver (84.7 ± 4.9%) and spleen (85.0 ± 3.1%) and hepatosplenomegaly by the artemisinin-loaded SLNs treated at 20 mg/kg compared to the free artemisinin. Therefore, the present study supports the superior efficacy of artemisinin-loaded SLNs over the free artemisinin and could be considered as a new therapeutic strategy in the treatment of leishmaniasis.

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来源期刊
Pathogens and Global Health
Pathogens and Global Health PUBLIC, ENVIRONMENTAL & OCCUPATIONAL HEALTH-PARASITOLOGY
CiteScore
6.00
自引率
0.00%
发文量
60
审稿时长
6-12 weeks
期刊介绍: Pathogens and Global Health is a journal of infectious disease and public health that focuses on the translation of molecular, immunological, genomics and epidemiological knowledge into control measures for global health threat. The journal publishes original innovative research papers, reviews articles and interviews policy makers and opinion leaders on health subjects of international relevance. It provides a forum for scientific, ethical and political discussion of new innovative solutions for controlling and eradicating infectious diseases, with particular emphasis on those diseases affecting the poorest regions of the world.
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