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木犀草素-磷脂复合物:制备、表征及生物学评价。

Luteolin-phospholipid complex: preparation, characterization and biological evaluation.

作者信息

Khan Junaid, Alexander Amit, Saraf Swarnlata, Saraf Shailendra

机构信息

University Institute of Pharmacy, Pandit Ravishankar Shukla University, Raipur, Chhattisgarh, India.

出版信息

J Pharm Pharmacol. 2014 Oct;66(10):1451-62. doi: 10.1111/jphp.12280. Epub 2014 Jun 16.

Abstract

OBJECTIVES

This study aims to develop novel carrier system incorporating luteolin, a poorly soluble biologically active plant active.

METHODS

We investigated a lipid-based drug delivery system to enhance dissolution and absorption profile of luteolin. Luteolin was complexed with phospholipids, and the preparation was characterized. The formulation was evaluated for physicochemical properties, in-vitro solubility or release studies. In vivo anti-inflammatory action of luteolin and its phospholipid complex was evaluated by using carrageenan and 12-O-tetradecanoylphorbol-13-acetate as inducers.

KEY FINDINGS

The prepared luteolin-phospholipid complex (LPC) showed drug loading of about 72.64% with average particle size of 152.6 nm. The Fourier transform infrared spectroscopy and thermal studies confirm formation of complex. The solubility of luteolin as LPC was about 2.5 times higher than the solubility of pure luteolin in water. In the diffusion study, LPC showed 95.12% of drug release at the end of 2 h. Animal studies demonstrated significant differences in response of LPC and luteolin.

CONCLUSION

LPC was successfully prepared by optimizing the process parameters. The resultant delivery system improved bioavailability and efficacy of luteolin and in the future may become an efficient tool for administration of luteolin.

摘要

目的

本研究旨在开发一种新型载体系统,该系统包含木犀草素,一种难溶性生物活性植物成分。

方法

我们研究了一种基于脂质的药物递送系统,以提高木犀草素的溶解和吸收情况。木犀草素与磷脂形成复合物,并对该制剂进行表征。对该制剂进行了理化性质、体外溶解度或释放研究的评估。以角叉菜胶和十四酰佛波醇乙酯为诱导剂,评估了木犀草素及其磷脂复合物的体内抗炎作用。

主要发现

制备的木犀草素 - 磷脂复合物(LPC)的载药量约为72.64%,平均粒径为152.6纳米。傅里叶变换红外光谱和热分析证实了复合物的形成。木犀草素作为LPC在水中的溶解度约为纯木犀草素溶解度的2.5倍。在扩散研究中,LPC在2小时结束时显示出95.12%的药物释放。动物研究表明LPC和木犀草素的反应存在显著差异。

结论

通过优化工艺参数成功制备了LPC。所得递送系统提高了木犀草素的生物利用度和疗效,未来可能成为木犀草素给药的有效工具。

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