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负载Q10的纳米脂质载体与纳米乳剂:稳定性、流变学及体外皮肤渗透

Q10-loaded NLC versus nanoemulsions: stability, rheology and in vitro skin permeation.

作者信息

Junyaprasert Varaporn B, Teeranachaideekul Veerawat, Souto Eliana B, Boonme Prapaporn, Müller Rainer H

机构信息

Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Thailand.

出版信息

Int J Pharm. 2009 Jul 30;377(1-2):207-14. doi: 10.1016/j.ijpharm.2009.05.020. Epub 2009 May 22.


DOI:10.1016/j.ijpharm.2009.05.020
PMID:19465098
Abstract

In this study, nanoemulsions (NE) of medium chain triacylglycerols (MCT) and nanostructured lipid carriers (NLC) of cetyl palmiate/MCT were produced to load coenzyme Q(10) (Q(10)) and characterized for their stability before and after incorporation into xanthan gum hydrogels. After storage at 4, 25 and 40 degrees C, the particles remained in the nanosize range for 12 months, with zeta potential higher than |40 mV|. Similar results were found in xanthan gum-based hydrogels containing NE or NLC. The crystallinity index of Q(10)-loaded NLC increased after being incorporated into hydrogels. The Q(10) entrapped in NLC and NE remained higher than 90% at all temperatures for 12 months but dramatically decreased when exposed to light. From the rheological studies, both NLC and NE dispersions possessed pseudoplastic flow having more liquid characteristics, whereas NLC and NE hydrogels exhibited plastic flow with thixothopy, showing more elastic rather than viscous properties. The occurrence of a spatial arrangement of lipid molecules was observed in the matrix of NLC when entrapped into hydrogels. From in vitro permeation studies, it could be stated that the amount of Q(10) released and occlusiveness were major keys to promote the deep penetration of Q(10) into the skin.

摘要

在本研究中,制备了中链三酰甘油(MCT)的纳米乳剂(NE)以及棕榈酸十六酯/MCT的纳米结构脂质载体(NLC)来负载辅酶Q(10)(Q(10)),并对其在掺入黄原胶水凝胶前后的稳定性进行了表征。在4℃、25℃和40℃储存后,颗粒在12个月内保持纳米尺寸范围,zeta电位高于|40 mV|。在含有NE或NLC的黄原胶基水凝胶中也发现了类似结果。负载Q(10)的NLC掺入水凝胶后,其结晶度指数增加。NLC和NE中包封的Q(10)在所有温度下12个月内均保持高于90%,但在光照下显著降低。流变学研究表明,NLC和NE分散体均具有假塑性流动,具有更多的液体特性,而NLC和NE水凝胶则表现出具有触变性的塑性流动,显示出更多的弹性而非粘性特性。当NLC包封在水凝胶中时,在其基质中观察到脂质分子的空间排列。体外渗透研究表明,Q(10)的释放量和封闭性是促进Q(10)深入皮肤的关键因素。

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