Department of Petroleum and Chemical Engineering, Science and Research Branch, Islamic Azad University, Tehran, Iran.
Department of Petroleum and Chemical Engineering, Science and Research Branch, Islamic Azad University, Tehran, Iran.
Chem Phys Lipids. 2022 Jul;245:105180. doi: 10.1016/j.chemphyslip.2022.105180. Epub 2022 Mar 2.
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 IC of free AmB is 4.834 µg/ml, while the nano-diameter AmB has a significantly lower IC 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.
疟疾是全世界热带和亚热带地区最具挑战性的寄生虫感染性疾病之一。恶性疟原虫的耐药性不断增加,使得疟疾的治疗过程更加具有挑战性和问题。因此,开发新的抗疟药物对于有效治疗至关重要。在这项研究中,研究人员将包裹在 DSPC/DSPE-PEG2000 胶束中的两性霉素 B(Constantinides 等人)作为一种抗疟药物,用于抗恶性疟原虫 3D7 株。通过 DLS、FESEM 和 TEM 分析,测定了无药物和载药胶束的平均粒径、形态和微观结构特性。合成的载有两性霉素 B 的磷脂胶束平均粒径为 115nm,多分散指数为 0.331。TEM 和 SEM 研究表明胶束具有均匀和均匀的形态。药物包封效率为 88.3%。胶束体系的缓慢释放表明,在 24 小时内最大药物释放量为 75.67%。这项体外研究是在恶性疟原虫 3D7 上进行的,旨在研究 AmB 胶束与恶性疟原虫寄生虫之间的相互作用,使用了不同的药物比例。根据研究结果,游离 AmB 的 IC 为 4.834µg/ml,而纳米直径的 AmB 的 IC 显著降低至 2.394µg/ml。研究结果表明,载药磷脂胶束的生物活性明显高于游离 AmB,对恶性疟原虫的杀伤作用更强。此外,根据这项研究的结果,载药的磷脂胶束是治疗疟疾的有前途的纳米结构。因此,纳米包裹的 AmB 显示出治疗疟疾的应用前景。