载两性霉素B的新型磷脂胶束对恶性疟原虫原生动物的体外研究

IF 3.4 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Khadijeh Rajablou , Hossein Attar , Seyed Kazem Sadjady , Amir Heydarinasab
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引用次数: 1

摘要

疟疾是全球热带和亚热带地区最具挑战性的寄生虫传染病之一。恶性疟原虫的耐药性日益增强,甚至使疟疾的治疗程序更具挑战性和更多的问题。因此,开发新的抗疟药物以进行有效治疗至关重要。本研究以DSPC/DSPE-PEG2000胶束包封的两性霉素B (Constantinides et al.)作为恶性疟原虫3D7菌株的抗疟药物进行了研究。用DLS、FESEM和TEM分析两性霉素B制备的无药胶束和载药胶束的平均粒径、形态和微观结构特性。合成的含AmB药物的磷脂胶束平均直径为115 nm,多分散性指数为0.331。透射电镜(TEM)和扫描电镜(SEM)研究表明,胶束形貌均匀均匀。药物包封率为88.3%。胶束体系的缓释效果较好,24 h内最大释药量为75.67%。本实验以恶性疟原虫3D7为实验对象,研究不同药物配比下AmB胶束与恶性疟原虫的相互作用。结果表明,游离AmB的IC50为4.834µg/ml,而纳米直径的AmB的IC50为2.394µg/ml。本研究结果表明,与直接施用AmB相比,载药磷脂胶束具有明显更高的生物活性和更强的疟原虫特性。此外,根据本研究的结果,包封的AmB药物是治疗疟疾的有前途的纳米结构。因此,纳米胶囊化AmB在疟疾治疗中具有广阔的应用前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The in-vitro study of novel phospholipid micelles loaded with amphotericin B on plasmodium falciparum protozoan

Malaria is one of the most challenging parasitic infectious diseases in tropical and subtropical regions all over the world. The increasing drug resistance of plasmodium falciparum even makes the treatment procedure of malaria challenging and more problematic. Therefore, it is essential to develop new antimalarial drugs for effective treatments. In this study, the encapsulated amphotericin B (Constantinides et al.) in DSPC/DSPE-PEG2000 micelles was investigated as an antimalarial drug against P. falciparum 3D7 strain. The mean particle size, morphological and microstructural properties of drug-free and drug-loaded micelles prepared with amphotericin B were determined through DLS, FESEM, and TEM analysis. The synthesized phospholipid micelles containing AmB drug with a mean diameter of 115 nm and a polydispersity index of 0.331. The TEM and SEM studies indicate the uniform and homogeneous morphology of the micelles. Drug encapsulation efficiency is 88.3%. The slow release of the micellar system shows the maximum drug release of 75.67% within 24 h. This in vitro study was conducted on P. falciparum 3D7 to investigate the interactions between AmB micelles and P. falciparum parasites using different drug ratios. According to the findings, the IC50 of free AmB is 4.834 µg/ml, while the nano-diameter AmB has a significantly lower IC50 of 2.394 µg/ml. The results of this study suggest that the drug-loaded phospholipid micelles have significantly higher bioactivity and greater plasmodial properties compared to the direct application of AmB against P. falciparum. Moreover, according to the results of this study, the encapsulated AmB drugs are promising nanostructures for malaria treatment. Therefore the nanoencapsulation AmB showed promising application for malaria treatment.

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来源期刊
Chemistry and Physics of Lipids
Chemistry and Physics of Lipids 生物-生化与分子生物学
CiteScore
7.60
自引率
2.90%
发文量
50
审稿时长
40 days
期刊介绍: Chemistry and Physics of Lipids publishes research papers and review articles on chemical and physical aspects of lipids with primary emphasis on the relationship of these properties to biological functions and to biomedical applications. Accordingly, the journal covers: advances in synthetic and analytical lipid methodology; mass-spectrometry of lipids; chemical and physical characterisation of isolated structures; thermodynamics, phase behaviour, topology and dynamics of lipid assemblies; physicochemical studies into lipid-lipid and lipid-protein interactions in lipoproteins and in natural and model membranes; movement of lipids within, across and between membranes; intracellular lipid transfer; structure-function relationships and the nature of lipid-derived second messengers; chemical, physical and functional alterations of lipids induced by free radicals; enzymatic and non-enzymatic mechanisms of lipid peroxidation in cells, tissues, biofluids; oxidative lipidomics; and the role of lipids in the regulation of membrane-dependent biological processes.
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