TY - JOUR
T1 - Pharmacological effect of a new idebenone formulation in a model of carrageenan-induced inflammatory pain
AU - Lauro, Filomena
AU - Ilari, Sara
AU - Giancotti, Luigino Antonio
AU - Ventura, Cinzia Anna
AU - Morabito, Chiara
AU - Gliozzi, Micaela
AU - Malafoglia, Valentina
AU - Palma, Ernesto
AU - Paolino, Donatella
AU - Mollace, Vincenzo
AU - Muscoli, Carolina
PY - 2016/9/1
Y1 - 2016/9/1
N2 - 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.
AB - 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.
KW - Antioxidant
KW - HP-β-cyclodextrins
KW - Idebenone
KW - Inflammatory pain
KW - Oxidative stress
UR - http://www.scopus.com/inward/record.url?scp=84980463782&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84980463782&partnerID=8YFLogxK
U2 - 10.1016/j.phrs.2016.07.043
DO - 10.1016/j.phrs.2016.07.043
M3 - Article
AN - SCOPUS:84980463782
SN - 1043-6618
VL - 111
SP - 763
EP - 767
JO - Pharmacological Research
JF - Pharmacological Research
ER -