Dewi Mayang Kusuma, Muhaimin Muhaimin, Joni I Made, Hermanto Faizal, Chaerunisaa Anis Yohana
Doctoral Program in Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, Indonesia.
Department of Pharmaceutical Biology, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, Indonesia.
Int J Nanomedicine. 2024 Sep 11;19:9411-9435. doi: 10.2147/IJN.S467811. eCollection 2024.
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 and developing a predictive model to enhance its antimalarial activity.
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 using Peter's 4-day suppressive test.
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 () 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 extract and fraction alone.
The findings indicated that the vesicular formulation in phytosomes can enhance the antimalarial activity of extract and fraction.
提取物具有抗疟活性，主要归因于其次生代谢产物——萘醌、黄酮类化合物、单宁和皂苷，其中萘醌是主要活性成分。然而，其低生物利用度限制了其有效性。为改善这一情况，提出了一种基于植物脂质体的囊泡系统。本研究着重于用[提取物名称]制备植物脂质体并开发预测模型以增强其抗疟活性。
采用反溶剂沉淀法制备植物脂质体，并用三因素、三水平的Box-Behnken模型进行优化。评估了粒径、zeta电位和包封率。通过其物理性质和释放曲线对优化后的植物脂质体进行表征。使用彼得4天抑制试验在感染[疟原虫名称]的白色BALB/c小鼠中测试其抗疟活性。
最佳植物脂质体制剂的磷脂与提取物比例为1:3，回流温度为50°C，持续时间为2.62小时。植物脂质体的粒径为471.8 nm，zeta电位为-54.1 mV，包封率（EE）为82.4%。相比之下，植物脂质体-级分的粒径为233.4 nm，zeta电位为-61.5 mV，EE为87.08%。透射电镜分析证实两者均为球形。植物脂质体-提取物在24小时的体外释放率为86.2%，植物脂质体-级分为95.9%，而单独的提取物和级分分别为46.9%和37.7%。总体而言，植物脂质体制剂表现出良好的稳定性。实际实验值与Box-Behnken模型的预测值紧密匹配，表明该模型具有高度准确性。此外，植物脂质体表现出比单独的[提取物名称]提取物和级分显著更高的抗疟活性。
研究结果表明，植物脂质体中的囊泡制剂可增强[提取物名称]提取物和级分的抗疟活性。
