Fabrication of Phytosome with Enhanced Activity of Sonneratia alba: Formulation Modeling and in vivo Antimalarial Study

IF 6.6 2区医学 Q1 NANOSCIENCE & NANOTECHNOLOGY

International Journal of Nanomedicine Pub Date : 2024-09-11 DOI:10.2147/ijn.s467811

Mayang Kusuma Dewi, Muhaimin Muhaimin, I Made Joni, Faizal Hermanto, Anis Yohana Chaerunisaa

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引用次数: 0

Abstract

Introduction: Sonneratia alba extract exhibits antimalarial activity, mainly due to its secondary metabolites—naphthoquinones, flavonoids, tannins, and saponins—where naphthoquinone is the primary active component. However, its low bioavailability limits its effectiveness. To improve this, a phytosome-based vesicular system was proposed. This study focused on formulating a phytosome with S. alba and developing a predictive model to enhance its antimalarial activity.
Methods: Phytosomes were produced using antisolvent precipitation and optimized with 3-factor, 3-level Box-behnken model. Particle size, zeta potential, and entrapment efficiency were assessed. The optimized phytosomes were characterized by their physical properties and release profiles. Their antimalarial activity was tested in white BALB/c mice infected with Plasmodium berghei using Peter’s 4-day suppressive test.
Results: The optimal phytosome formulation used a phospholipid-to-extract ratio of 1:3, reflux temperature of 50°C, and a duration of 2.62 hours. The phytosomes had a particle size of 471.8 nm, a zeta potential of − 54.1 mV, and an entrapment efficiency (EE) of 82.4%. In contrast, the phytosome-fraction showed a particle size of 233.4 nm, a zeta potential of − 61.5 mV, and an EE of 87.08%. TEM analysis confirmed both had a spherical shape. In vitro release rates at 24 hours were 86.2 for the phytosome-extract and 95.9% for the phytosome-fraction, compared to 46.9% and 37.7% for the extract and fraction alone. Overall, the phytosome formulation demonstrated good stability. The actual experimental values closely matched the predicted values from the Box–Behnken model, indicating a high degree of accuracy in the model. Additionally, the phytosomes exhibited significantly greater antimalarial activity than the S. alba extract and fraction alone.
Conclusion: The findings indicated that the vesicular formulation in phytosomes can enhance the antimalarial activity of S. alba extract and fraction.

Keywords: antimalarial S.alba, phytosome, box-behnken, extract, fraction

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制造具有增强白桑子活性的植物胶囊：配方建模和体内抗疟研究

简介：白桑子提取物具有抗疟活性，这主要归功于它的次生代谢物--萘醌、黄酮、单宁和皂苷，其中萘醌是主要的活性成分。然而，萘醌的生物利用率较低，限制了它的功效。为了改善这种情况，有人提出了一种基于植物激素的囊泡系统。本研究的重点是用白藜芦醇配制植物囊体，并建立一个预测模型以提高其抗疟活性：方法：使用反溶剂沉淀法生产植物囊体，并使用 3 因子、3 级 Box-behnken 模型进行优化。评估了粒度、ZETA电位和夹带效率。对优化后的植物载体的物理性质和释放曲线进行了表征。利用彼得氏 4 天抑制试验，在感染了伯格氏疟原虫的白色 BALB/c 小鼠身上测试了它们的抗疟活性：最佳植物胶体配方的磷脂与提取物的比例为 1:3，回流温度为 50°C，持续时间为 2.62 小时。植物体的粒径为 471.8 纳米，zeta 电位为 - 54.1 mV，夹带效率（EE）为 82.4%。相比之下，植物体馏分的粒径为 233.4 nm，zeta 电位为 - 61.5 mV，EE 为 87.08%。TEM 分析证实两者都呈球形。在 24 小时的体外释放率方面，植物提取物为 86.2%，植物馏分为 95.9%，而单独使用提取物和馏分的释放率分别为 46.9% 和 37.7%。总体而言，植物胶囊制剂表现出良好的稳定性。实际实验值与 Box-Behnken 模型的预测值非常吻合，表明该模型具有很高的准确性。此外，植物体的抗疟活性明显高于单独的白藜芦醇提取物和馏分：结论：研究结果表明，植物体中的囊状配方可以增强白僵菌提取物和馏分的抗疟活性。关键词：白僵菌；植物体；Box-behnken；提取物；馏分

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来源期刊

International Journal of Nanomedicine NANOSCIENCE & NANOTECHNOLOGY-PHARMACOLOGY & PHARMACY

CiteScore

14.40

自引率

3.80%

发文量

511

审稿时长

1.4 months

期刊介绍： The International Journal of Nanomedicine is a globally recognized journal that focuses on the applications of nanotechnology in the biomedical field. It is a peer-reviewed and open-access publication that covers diverse aspects of this rapidly evolving research area. With its strong emphasis on the clinical potential of nanoparticles in disease diagnostics, prevention, and treatment, the journal aims to showcase cutting-edge research and development in the field. Starting from now, the International Journal of Nanomedicine will not accept meta-analyses for publication.