4.3 Article

The in-vitro study of novel phospholipid micelles loaded with amphotericin B on plasmodium falciparum protozoan

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CHEMISTRY AND PHYSICS OF LIPIDS
卷 245, 期 -, 页码 -

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ELSEVIER IRELAND LTD
DOI: 10.1016/j.chemphyslip.2022.105180

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Amphotericin B; Phospholipid micelle; Drug encapsulation; Plasmodium falciparum; Malaria

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Malaria is a challenging parasitic infectious disease in tropical and subtropical regions. This study investigates the potential of encapsulated amphotericin B as an antimalarial drug and its higher bioactivity against P. falciparum 3D7 strain.
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 mu g/ml, while the nano-diameter AmB has a significantly lower IC50 of 2.394 mu g/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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