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

Journal of drug delivery Pub Date : 2018-06-03 eCollection Date: 2018-01-01 DOI:10.1155/2018/2908626
P Vijayanand, V Jyothi, N Aditya, A Mounika
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引用次数: 17

Abstract

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.

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含有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。
在阿育吠陀和传统中医等替代医学体系中,芙蓉及其提取物传统上因其抗抑郁活性而被处方。粗提取物和基本配方方法有利于概念验证研究;然而,这些配方充满了诸如口服生物利用度差和受试者之间的高度可变性等问题。系统给药方法在解决其中一些问题方面可能被证明是有效的。在这项研究中,我们报道了以单硬脂酸甘油或蜂蜡为脂质负载固体脂质纳米颗粒(hsln)的芙蓉提取物的开发。对hsln的大小、表面电荷和形态进行了评价。在雄性瑞士白化小鼠中测试了优化后的hsln的抗抑郁活性。结果表明,在优化的工艺条件下,可以得到~175 nm的带负电荷的近球形hsln。体内实验结果表明,实验动物的静止时间有显著差异。此外,hsln在比天然粗提物低几倍的剂量下,也能获得类似的药理作用。这些初步研究结果表明,将植物药包封到先进的输送系统中,如固体脂质纳米颗粒,可能是改善其体内性能的有效策略。
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Journal of drug delivery
Journal of drug delivery PHARMACOLOGY & PHARMACY-
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