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Development and Characterization of Solid Lipid Nanoparticles Containing Herbal Extract: In Vivo Antidepressant Activity

机译:含草药提取物的固体脂质纳米颗粒的开发和表征:体内抗抑郁活性。

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摘要

In alternate systems of medicine like Ayurveda and traditional Chinese medicine, Hibiscus rosa sinensis and its extracts have been traditionally prescribed for their antidepressant activity. Crude extracts and rudimentary formulations approaches are good for proof-of-concept studies; however, these formulations are fraught with problems like poor oral bioavailability and high variability between subjects. Systematic drug delivery approaches could prove effective in addressing some of these problems. In this study, we report the development of Hibiscus rosa sinensis extract loaded solid lipid nanoparticles (HSLNs) using glycerol monostearate or beeswax as lipids. The HSLNs were evaluated for their size, surface charge, and morphology. The optimized HSLNs were tested for antidepressant activity in male Swiss albino mice. It was found that, with the optimized procedure, HSLNs of ~175 nm, carrying negative charge and nearly spherical shape, could be obtained. The in vivo test results suggested that there were marked differences in the immobility times of the test animals. Moreover, with HSLNs, it was found that at doses several times lower than the native crude extract dose, similar pharmacological effect could be obtained. These initial findings suggest that encapsulating phytopharmaceuticals into advanced delivery systems like solid lipid nanoparticles can be an effective strategy in improving their in vivo performance.
机译:在阿育吠陀和传统中草药等替代医学体系中,传统上已开处方了芙蓉罗莎及其提取物的抗抑郁活性。粗提物和基本配方方法非常适合概念验证研究;然而,这些制剂存在诸如口服生物利用度差和受试者之间差异大等问题。系统的药物输送方法可以有效解决其中一些问题。在这项研究中,我们报告使用单硬脂酸甘油酯或蜂蜡作为脂质的芙蓉罗莎提取物固体脂质纳米粒(HSLNs)的开发。评估了HSLN的大小,表面电荷和形态。测试了优化的HSLN在雄性瑞士白化病小鼠中的抗抑郁活性。结果发现,通过优化程序,可以获得带有负电荷且近似球形的〜175 nm HSLN。体内测试结果表明测试动物的固定时间存在明显差异。此外,使用HSLNs,发现其剂量比天然粗提取物剂量低几倍,可以获得类似的药理作用。这些初步发现表明,将植物药物包封到先进的递送系统(如固体脂质纳米颗粒)中可以是提高其体内性能的有效策略。

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