芥蓝抗炎、抗焦虑、抗氧化性能及微球负载缓释抗炎凝胶的制备

R. Gyawali, A. Ghimire, Apeksha Khatiwada, Prakshit Niraula, U. Sharma, Roshan Thapa
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摘要

分别采用福尔马林致小鼠足跖水肿试验和升高+迷宫动物模型,评价苜蓿提取物的抗炎和抗焦虑作用。采用水包油包水复合乳液体系,再采用溶剂蒸发法制备了含有分散提取物的固体微球。使用Minitab 16进行优化,并将优化后的微球装入凝胶基中。采用DPPH(2,2-二苯基-苦味酰肼)测定法对优化后的微球负载凝胶的抗氧化活性进行了评价。通过福尔马林诱导小鼠足跖水肿试验,对凝胶的物理性能、药物释放动力学和抗炎活性进行了评估,并将其抗炎潜能与市售双氯芬酸凝胶(1.16% w/w)进行了比较。各剂量提取物及微球负载缓释抗炎凝胶对水肿均有剂量依赖性和时间依赖性的抑制作用(P<0.05),对焦虑水平也有剂量依赖性的抑制作用(P<0.001)。对不同浓度的粗提物和微球凝胶进行了潜在的抗氧化活性研究。抗坏血酸、甲醇提取物和微球凝胶的IC50值分别为5.62 μg/mL、6.34 μg/mL和8.25 μg/mL。
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Anti-inflammatory, Anxiolytic and Antioxidant Property of Lactuca sativa L and Formulation of Microspheres Loaded Sustained Release Anti-inflammatory Gel
Anti-inflammatory and anxiolytic properties of Lactuca sativa L extract was evaluated by formalin induced mice paw edema test, and elevated plus maze animal model respectively. Solid microspheres containing dispersed extract were obtained by water-in-oil-in-water multiple emulsion system followed by solvent evaporation method. Optimization was carried out using Minitab 16 and optimized microspheres were loaded into a gel base. Anti-oxidant activity of optimized microspheres loaded gel was evaluated using DPPH (2,2-diphenyl1-picrylhydrazyl) assay. The gel was also evaluated for its physical properties, drug release kinetics and antiinflammatory activity using formalin induced mice-paw edema test where the anti-inflammatory potential was compared to marketed diclofenac gel (1.16% w/w). All doses of extract as well as microsphere loaded sustained release anti-inflammatory gel showed a dose and time dependent inhibition of edema (P<0.05), the extract also showed a dose dependent inhibition of level of anxiety (P<0.001). Potential anti-oxidant activity was seen with different concentration of crude extract and microsphere loaded gel. The anti-oxidant potential was compared using IC50 value which was 5.62 μg/mL, 6.34 μg/mL, 8.25 μg/mL for ascorbic acid, methanolic extract of L. sativa and microspheres loaded gel respectively.
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