title: Protective role of free and quercetin-loaded nanoemulsion against damage induced by intracerebral haemorrhage in rats.
abstract: Intracerebral haemorrhage (ICH) is a worldwide public health problem. Experimental studies have shown that oxidative stress plays an important role in the pathogenesis of ICH and could represent a target for its treatment. However, the blood-brain barrier is an obstacle to be overcome, as it hampers the administration of compounds to the central nervous system. In this study, we compared the effects of a quercetin-loaded nanoemulsion (QU-N) with the free form of the drug (QU-SP) in a collagenase-induced ICH rat model. Quercetin (QU) is a polyphenol that has an antioxidant effect in vitro, but due to its high lipophilicity, it has low bioavailability in vivo. In this study, animals submitted or not to ICH were treated with a single intraperitoneal QU dose (free or nanoemulsion) of 30 mg kg(-1). Motor assessment was evaluated by the open field, foot fault and beam walking behavioural tests. 72 h after surgery the haematoma size was evaluated and biochemical measurements were performed. Animals treated with QU-N had a significant improvement in the beam walking and open field tests. Also, QU-N was able to reduce the size of the haematoma, preserving the activity of glutathione S-transferase (GST), increasing GSH content, and the total antioxidant capacity. QU-SP recovered locomotor activity and increased the GSH content and the total antioxidant capacity. Thus, it can be observed that QU presented antioxidant activity in both formulations, but the incorporation into nanoemulsions increased its antioxidant effect, which was reflected in the improvement of the motor skills and in the haematoma size decrement. These results suggest that the nanoemulsion containing QU developed in this study could be promising for future studies on treatments for ICH.
authors.affiliation: Programa de Pós-graduação em Ciências Fisiológicas - Fisiologia Animal Comparada, Universidade Federal do Rio Grande (FURG), Rio Grande, RS, 96210-900, Brazil.
authors.forename: A R
authors.initials: AR
authors.lastname: Galho
authors.forename: M F
authors.initials: MF
authors.lastname: Cordeiro
authors.forename: S A
authors.initials: SA
authors.lastname: Ribeiro
authors.forename: M S
authors.initials: MS
authors.lastname: Marques
authors.forename: M F D
authors.initials: MF
authors.lastname: Antunes
authors.forename: D C
authors.initials: DC
authors.lastname: Luz
authors.forename: G
authors.initials: G
authors.lastname: Hädrich
authors.forename: A L
authors.initials: AL
authors.lastname: Muccillo-Baisch
authors.forename: D M
authors.initials: DM
authors.lastname: Barros
authors.forename: J V
authors.initials: JV
authors.lastname: Lima
authors.forename: C L
authors.initials: CL
authors.lastname: Dora
authors.forename: A P
authors.initials: AP
authors.lastname: Horn
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D001835:Body Weight / Q000187:drug effects; D002543:Cerebral Hemorrhage / Q000188:drug therapy* / Q000209:etiology; D002851:Chromatography, High Pressure Liquid; D017364:Collagenases / Q000378:metabolism; D004195:Disease Models, Animal; D004337:Drug Carriers / Q000737:chemistry*; D004655:Emulsions / Q000737:chemistry; D005978:Glutathione / Q000378:metabolism; D005982:Glutathione Transferase / Q000378:metabolism; D008124:Locomotion / Q000187:drug effects; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D011794:Quercetin / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar
chemical_list: D000975:Antioxidants; D004337:Drug Carriers; D004655:Emulsions; D011794:Quercetin; D005982:Glutathione Transferase; D017364:Collagenases; D005978:Glutathione