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含草药提取物的固体脂质纳米粒的研制与表征:体内抗抑郁活性

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

作者信息

Vijayanand P, Jyothi V, Aditya N, Mounika A

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, M. S. Ramaiah University of Applied Sciences, Bengaluru 560054, Karnataka, India.

Sri Venkateshwara College of Pharmacy, Madhapur, Hyderabad 500081, India.

出版信息

J Drug Deliv. 2018 Jun 3;2018:2908626. doi: 10.1155/2018/2908626. eCollection 2018.

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 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 performance.

摘要

在阿育吠陀和传统中医等替代医学体系中,朱槿及其提取物传统上因其抗抑郁活性而被使用。粗提物和初级制剂方法适用于概念验证研究;然而,这些制剂存在口服生物利用度差和个体间差异大等问题。系统性给药方法可能在解决其中一些问题方面证明是有效的。在本研究中,我们报告了以单硬脂酸甘油酯或蜂蜡为脂质制备负载朱槿提取物的固体脂质纳米粒(HSLNs)。对HSLNs的尺寸、表面电荷和形态进行了评估。对优化后的HSLNs在雄性瑞士白化小鼠中进行抗抑郁活性测试。结果发现,通过优化工艺,可以获得尺寸约为175nm、带负电荷且近似球形的HSLNs。测试结果表明,试验动物的不动时间存在显著差异。此外,使用HSLNs发现,在剂量比天然粗提物剂量低几倍的情况下,仍可获得相似的药理效果。这些初步发现表明,将植物药封装到固体脂质纳米粒等先进给药系统中可能是提高其性能的有效策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6e9/6008679/c5f3b8debb5f/JDD2018-2908626.001.jpg

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