Pharmacological effect of a new idebenone formulation in a model of carrageenan-induced inflammatory pain

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• 作者：Filomena Lauro^a ; Sara Ilari^a ; Luigino Antonio Giancotti^a ; Cinzia Anna Ventura^b ; Chiara Morabito^c ; Micaela Gliozzi^d ; Valentina Malafoglia^e ; Ernesto Palma^d ; Donatella Paolino^f ; Vincenzo Mollace^d ; Carolina Muscoli^d ; ^{muscoli@unicz.it" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Inflammatory pain ; Oxidative stress ; Antioxidant ; Idebenone ; HP-β-cyclodextrins
• 刊名：Pharmacological Research
• 出版年：2016
• 出版时间：September 2016
• 年：2016
• 卷：111
• 期：Complete
• 页码：767-773
• 全文大小：920 K

文摘

Considerable evidence demonstrated that the central role of reactive oxygen species and reactive nitrogen species (ROS and RNS) in the development of thermal hyperalgesia is associated to acute and chronic inflammation.

Idebenone (IDE), a synthetic analogue of the endogenous cellular antioxidant coenzyme Q10 (CoQ10), is an active drug in the central nervous system which shows a protection in a variety of neurological disorders. Since it is lipophilic, poorly water soluble and highly bound to plasma proteins, different technological approaches have been explored to increase its solubility and new pharmaceutical properties. Therefore, it has been complexed with HP-β-cyclodextrins (HP) and its efficacy has been assessed in an animal model of carrageenan-induced thermal hyperalgesia.

All male rats used for this study received a subplantar injection of carrageenan into the right hindpaw in the presence or absence of IDE alone and IDE/HP complex. We observed that IDE poorly reduced painful carrageenan effects whereas IDE/HP complex was able to prevent carrageenan-induced hyperalgesia and edema in a dose-dependent manner, reducing spinal MDA levels and protein nitration.

Hence, our results demonstrated that when complexed with HP, idebenone exerts a potent analgesic and anti-inflammatory efficacy.