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新型青蒿素投药方式:在实验内脏利什曼病中的生产与疗效。

A novel outlook in the delivery of artemisinin: production and efficacy in experimental visceral leishmaniasis.

机构信息

Department of Parasitology and mycology, Shiraz University of Medical Sciences, Shiraz, Iran.

Department of Nanomedicine, School of Advanced Medical Sciences and Technologies, Shiraz University of Medical Sciences, Shiraz, Iran.

出版信息

Pathog Glob Health. 2024 Feb;118(1):40-46. doi: 10.1080/20477724.2023.2212347. Epub 2023 May 15.

DOI:10.1080/20477724.2023.2212347
PMID:37183476
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10769112/
Abstract

The visceral form of leishmaniasis (VL), due to infection by , 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 -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.

摘要

内脏利什曼病(VL)是由 引起的一种被忽视的热带病。现有的治疗方法选择有限。青蒿素是一种有效的抗利什曼原虫药物,但生物利用度差,需要在 VL 中重复高剂量治疗。固体脂质纳米粒(SLNs)提供靶向递送,增加生物利用度并降低传统治疗策略的毒性。载青蒿素的 SLNs 呈球形,粒径为 222.0 ± 14.0nm。SLNs 对寄生虫没有特殊的毒性作用,而天然青蒿素在浓度为 250μg/ml 时对前鞭毛体的存活率表现出显著的毒性,毒性率为 31%。本研究在 -感染的 BALB/c 小鼠中进行了实验性 VL 中,证明了载青蒿素 SLNs 的治疗效果。与游离青蒿素相比,载青蒿素 SLNs 的 10 和 20mg/kg 剂量显示出更高的抗利什曼原虫疗效。与游离青蒿素相比,20mg/kg 载青蒿素 SLNs 治疗后,肝脏(84.7±4.9%)和脾脏(85.0±3.1%)中的寄生虫负荷和肝脾肿大明显减少。因此,本研究支持载青蒿素 SLNs 优于游离青蒿素的疗效,可考虑作为治疗利什曼病的新治疗策略。

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Immunotherapy in treatment of leishmaniasis.免疫疗法治疗利什曼病
Immunol Lett. 2021 May;233:80-86. doi: 10.1016/j.imlet.2021.03.011. Epub 2021 Mar 23.
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Applications of Nanomaterials in Leishmaniasis: A Focus on Recent Advances and Challenges.纳米材料在利什曼病中的应用:聚焦最新进展与挑战
Nanomaterials (Basel). 2019 Dec 9;9(12):1749. doi: 10.3390/nano9121749.
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Lipid nanoparticles for amphotericin delivery in the treatment of American tegumentary leishmaniasis.脂质纳米粒用于两性霉素递送治疗美洲皮肤利什曼病。
Drug Deliv Transl Res. 2020 Apr;10(2):403-412. doi: 10.1007/s13346-019-00677-4.
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A new multi-epitope peptide vaccine induces immune responses and protection against Leishmania infantum in BALB/c mice.一种新型多表位肽疫苗诱导 BALB/c 小鼠对利什曼原虫的免疫应答和保护。
Med Microbiol Immunol. 2020 Feb;209(1):69-79. doi: 10.1007/s00430-019-00640-7. Epub 2019 Nov 6.
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Curr Pharm Des. 2017 Nov 21. doi: 10.2174/1381612823666171122111132.
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Nanostructured delivery systems with improved leishmanicidal activity: a critical review.具有增强杀利什曼原虫活性的纳米结构递送系统:一项批判性综述。
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