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非离子表面活性剂囊泡增强叶黄素的透皮传递:质量评价和抗关节炎评估。

Enhanced transdermal delivery of luteolin via non-ionic surfactant-based vesicle: quality evaluation and anti-arthritic assessment.

机构信息

a Department of Pharmacognosy and Phytochemistry and.

b Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard University , New Delhi , India.

出版信息

Drug Deliv. 2016;23(3):1079-84. doi: 10.3109/10717544.2014.945130. Epub 2014 Aug 12.

DOI:10.3109/10717544.2014.945130
PMID:25116512
Abstract

Luteolin (LUT) is a promising molecule with potential anti-arthritic activity. This investigation presents formulation and evaluation of niosomal transgel for enhanced transdermal delivery of LUT. Different non-ionic surfactants and vesicle compositions were employed for preparation of niosomes. The vesicle size analysis showed that all vesicles were in the range from 534.58 to 810.22 nm which favoured efficient transdermal delivery. The entrapment of LUT in vesicle was found to be higher in all surfactant. The developed formulation was proved significantly superior in terms of amount of drug permeation with an enhancement ratio of 2.66 when compared to a control formulation. The in vivo bioactivity studies revealed that the prepared niotransgel formulation of LUT was able to provide good anti-arthritic activity and the results were comparable to standard (diclofenac gel for anti-arthritic and analgesic). Finally, the results were confirmed through radiological analysis which proved that the prepared niotransgel was effectively able to treat arthritis and results were comparable with the standard formulation.

摘要

木樨草素(LUT)是一种有前途的分子,具有潜在的抗关节炎活性。本研究提出了一种用于增强 LUT 经皮传递的尼森体转胶体制剂及其评价。采用不同的非离子表面活性剂和囊泡组成来制备尼森体。囊泡大小分析表明,所有囊泡的粒径均在 534.58 至 810.22nm 范围内,有利于高效经皮传递。结果表明,所有表面活性剂都能使 LUT 的包封率提高。与对照制剂相比,所开发的制剂在药物渗透量方面具有显著优势,渗透量增加了 2.66 倍。体内生物活性研究表明,所制备的 LUT 尼森体凝胶具有良好的抗关节炎活性,结果与标准制剂(双氯芬酸钠凝胶抗关节炎和镇痛)相当。最后,通过放射学分析证实了所制备的尼森体凝胶能够有效治疗关节炎,结果与标准制剂相当。

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