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艾地苯醌衍生物负载型固体脂质纳米粒的体外抗氧化活性

In Vitro Antioxidant Activity of Idebenone Derivative-Loaded Solid Lipid Nanoparticles.

作者信息

Montenegro Lucia, Modica Maria N, Salerno Loredana, Panico Anna Maria, Crascì Lucia, Puglisi Giovanni, Romeo Giuseppe

机构信息

Department of Drug Sciences, University of Catania, V. le A. Doria 6, 95125 Catania, Italy.

出版信息

Molecules. 2017 May 27;22(6):887. doi: 10.3390/molecules22060887.

DOI:10.3390/molecules22060887
PMID:28555014
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6152785/
Abstract

Idebenone (IDE) has been proposed for the treatment of neurodegenerative diseases involving mitochondria dysfunctions. Unfortunately, to date, IDE therapeutic treatments have not been as successful as expected. To improve IDE efficacy, in this work we describe a two-step approach: (1) synthesis of IDE ester derivatives by covalent linking IDE to other two antioxidants, trolox (IDETRL) and lipoic acid (IDELIP), to obtain a synergic effect; (2) loading of IDE, IDETRL, or IDELIP into solid lipid nanoparticles (SLN) to improve IDE and its esters' water solubility while increasing and prolonging their antioxidant activity. IDE and its derivatives loaded SLN showed good physico-chemical and technological properties (spherical shape, mean particle sizes 23-25 nm, single peak in the size distribution, ζ potential values -1.76/-2.89 mV, and good stability at room temperature). In vitro antioxidant activity of these SLN was evaluated in comparison with free drugs by means of oxygen radical absorbance capacity (ORAC) test. IDETRL and IDELIP showed a greater antioxidant activity than IDE and encapsulation of IDE and its derivatives into SLN was able to prolong their antioxidant activity. These results suggest that loading IDETRL and IDELIP into SLN could be a useful strategy to improve IDE efficacy.

摘要

艾地苯醌（IDE）已被提议用于治疗涉及线粒体功能障碍的神经退行性疾病。不幸的是，迄今为止，IDE的治疗效果并不如预期那样成功。为了提高IDE的疗效，在这项工作中我们描述了一种两步法：（1）通过将IDE与另外两种抗氧化剂——生育三烯酚（IDETRL）和硫辛酸（IDELIP）共价连接来合成IDE酯衍生物，以获得协同效应；（2）将IDE、IDETRL或IDELIP负载到固体脂质纳米粒（SLN）中，以提高IDE及其酯类的水溶性，同时增强并延长它们的抗氧化活性。负载有IDE及其衍生物的SLN表现出良好的物理化学和工艺性质（球形、平均粒径23 - 25 nm、粒径分布呈单峰、ζ电位值为 -1.76 / -2.89 mV，且在室温下具有良好的稳定性）。通过氧自由基吸收能力（ORAC）测试，将这些SLN的体外抗氧化活性与游离药物进行了比较。IDETRL和IDELIP表现出比IDE更强的抗氧化活性，并且将IDE及其衍生物封装到SLN中能够延长它们的抗氧化活性。这些结果表明，将IDETRL和IDELIP负载到SLN中可能是提高IDE疗效的一种有用策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/9f9048353d78/molecules-22-00887-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/27b417d96e59/molecules-22-00887-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/eb3899d8531c/molecules-22-00887-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/69862b9e14c6/molecules-22-00887-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/383561957e44/molecules-22-00887-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/c96ba2ba8856/molecules-22-00887-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/693cebc8563c/molecules-22-00887-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/a314a4aa596b/molecules-22-00887-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/030d3e17f740/molecules-22-00887-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/9f9048353d78/molecules-22-00887-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/27b417d96e59/molecules-22-00887-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/eb3899d8531c/molecules-22-00887-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/69862b9e14c6/molecules-22-00887-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/383561957e44/molecules-22-00887-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/c96ba2ba8856/molecules-22-00887-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/693cebc8563c/molecules-22-00887-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/a314a4aa596b/molecules-22-00887-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/030d3e17f740/molecules-22-00887-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b9c/6152785/9f9048353d78/molecules-22-00887-g008.jpg

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