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载伊文思蓝纳米脂质体的制备、表征及其对恶性疟原虫生长抑制作用的评价。

Preparation, characterization, and evaluation of eosin B-loaded nano-liposomes for growth inhibition of Plasmodium falciparum.

机构信息

Department of Biochemistry, Faculty of Biological Sciences, North Tehran Branch, Islamic Azad University, Tehran, Iran.

Department of Nanobiotechnology, New Technologies Research Group, Pasteur Institute of Iran, Tehran, Iran.

出版信息

Parasitol Res. 2022 Jan;121(1):383-393. doi: 10.1007/s00436-021-07395-2. Epub 2022 Jan 6.

Abstract

Malaria is a deadly disease in humans caused by the Plasmodium parasite. High prevalence of malaria and resistance of malaria parasite to currently proposed drugs have increased the need to introduce and use new and effective antimalarial agents. In this study, eosin B was used as an effective antimalarial agent, the efficacy of which has already been confirmed by in vitro models. Also, for efficacy and safety improvement of eosin B, liposomal nanocarrier was used because of diversity and adaptability in controlled drug delivery and targeting. Eosin B was trapped inside liposomal nanocarriers by thin layer hydration method and its optimization was performed based on size, polydispersity index, and drug entrapment efficiency. Finally, the eosin B-loaded liposomes were tested on Plasmodium falciparum in culture to evaluate its anti-plasmodial effect. According to the results, the formulation with DSPC:cholesterol 8:1 (molar ratio) and drug concentration of 3 mg/ml was selected as the optimal form. The optimal nano-liposomes showed a size of 163.3 nm, a polydispersity index of 0.250, and an encapsulation efficiency of 69.94%. The process of drug release from nanocarriers was also obtained about 63% at the end of 72 h. Stability studies over 2 months at 25 °C and 4 °C on the optimum sample showed that the samples stored in the refrigerator were more stable in terms of size characteristics, polydispersity index, and drug entrapment efficiency. The results indicate a greater effect of liposomal-formulated eosin B on inhibiting parasite growth compared to the free eosin B.

摘要

疟疾是一种由疟原虫引起的致命人类疾病。疟疾的高流行率和疟原虫对目前提议药物的耐药性增加了引入和使用新的有效抗疟药物的必要性。在这项研究中,曙红 B 被用作一种有效的抗疟药物,其疗效已通过体外模型得到证实。此外,为了提高曙红 B 的疗效和安全性,使用了脂质体纳米载体,因为它在药物控制释放和靶向方面具有多样性和适应性。曙红 B 通过薄层水化法被捕获在脂质体纳米载体中,并根据粒径、多分散指数和药物包封效率对其进行了优化。最后,在培养的疟原虫中测试了载有曙红 B 的脂质体,以评估其抗疟效果。结果表明,选择 DSPC:胆固醇 8:1(摩尔比)和药物浓度为 3 mg/ml 的制剂为最佳形式。最佳的纳米脂质体粒径为 163.3nm,多分散指数为 0.250,包封效率为 69.94%。还获得了纳米载体中药物释放的过程,在 72 小时结束时约为 63%。在 25°C 和 4°C 下对最佳样品进行了 2 个月的稳定性研究,结果表明,在冰箱中储存的样品在粒径特征、多分散指数和药物包封效率方面更稳定。结果表明,与游离曙红 B 相比,脂质体形式的曙红 B 对抑制寄生虫生长的效果更大。

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