ObjectiveTo develop and evaluate zolmitriptan spanlastics (Zol SLs) as a brain-targeted antimigraine delivery system. Spanlastics (SLs) prepared using span 60: tween 80 (70:30%, respectively) gave the highest percentage of entrapment efficiency (EE%).Materials and methodsA total of 60 adult male Wistar albino rats were divided into six groups (n=10 rats/group). Group 1 (Control) comprised rats serving as a negative control. Group 2 was treated with glyceryl trinitrate (NTG) and served as the positive control. Groups 3 (NTG+Zol com), Group 4 (NTG+Zol sol) and Group 5 (NTG+Zol SLs) received commercial zolmitriptan orally, zolmitriptan solution intranasally and Zol SLs F5 intranasally, respectively, 30 min before NTG. Group 6 (Zol SLs) comprised normal rats that received only Zol SLs intranasally.ResultsWe found decreased Tmax, increased Cmax, AUC0–6, AUC0–∞ and ameliorated behaviour in rats (head scratching) treated with intranasal SLs compared to oral commercial zolmitriptan.ConclusionOur study substantiates the enhanced efficacy of Zol SLs in brain targeting for migraine treatment.
Redox equilibrium is altered due to elevation of reactive oxygen species (ROS) or inadequate antioxidant defense, therapeutic effects of natural antioxidant such as curcumin (CMN) have been investigated. The aim of this study was to investigate the beneficial effects of curcumin (a natural polyphenol) on oxidative status of lung and liver and assessment of level of interleukin-6 (IL-6) in rats against paraquat toxicity. Forty adult male wistar rats were divided into five groups with eight animals each as followed: Group 1: control, Group 2: rats received olive oil. Group 3: rats received curcumin (CMN) (200 mg/kg body weight in olive oil) orally. Group 4 (model group): rats were given a single oral dose of paraquat (PQ) 50 mg/kg body weight dissolved in distilled water intra-peritoneally (I.P) Group 5: rats received CMN orally daily for 10 days prior to PQ administration with the same previous doses and after PQ. After forty eight hours of PQ administration, rats were sacrificed and lung and liver tissues samples were examined for detection of biochemical parameters and histopathological changes. Significant histopathological changes had resulted from PQ administration in lung and liver tissues in addition to significant increase in malondialdehyde (MDA), and significant decrease of catalase (CAT), superoxide dismutase (SOD) and glutathione reductase (GR). However, treatment with CMN produced increasing antioxidant markers and depletion of MDA compared to the model group. Also there is significant increase in serum IL-6 after PQ administration compared to control group. However, the level of IL-6 significantly decreased in treated group with curcumin compared to the model group. Curcumin possesses remarkable protection of the altered lung and liver tissues in paraquat intoxicated rats and could reduce the damaging effect by increasing antioxidant activity and decreasing lipid peroxidation, oxidative stress and IL-6.
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