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Molecules 2017, 22(6), 887; doi:10.3390/molecules22060887

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

Department of Drug Sciences, University of Catania, V. le A. Doria 6, 95125 Catania, Italy
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Author to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 1 May 2017 / Revised: 22 May 2017 / Accepted: 23 May 2017 / Published: 27 May 2017
(This article belongs to the Section Medicinal Chemistry)
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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. View Full-Text
Keywords: idebenone; lipoic acid; trolox; idebenone ester derivatives; antioxidant activity; ORAC idebenone; lipoic acid; trolox; idebenone ester derivatives; antioxidant activity; ORAC
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Montenegro, L.; Modica, M.N.; Salerno, L.; Panico, A.M.; Crascì, L.; Puglisi, G.; Romeo, G. In Vitro Antioxidant Activity of Idebenone Derivative-Loaded Solid Lipid Nanoparticles. Molecules 2017, 22, 887.

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