DEVELOPMENT AND IN-VITRO EVALUATION OF PHYTOSOMES CONTAINING HERBAL EXTRACT OF CENTELLA ASIATICA FOR ANTIULCER AND ANTIOXIDANT ACTIVITY

Baljeet Kaur, A. Saxena, Kirti Roy, M. Bhardwaj, M. Bisht
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Abstract

Herbal medications have a diverse range of active constituents allowing us to use them in a variety of ways, but active constituents are poorly absorbed due to their strong polarity and low lipophilicity, resulting in low bioavailability. The aim of this research was to improve bioavailability by development and in-vitro evaluation of phytosomes containing herbal extract of Centella asiatica for its antioxidant and gastroprotective activity. Phytosomes of Centella asiatica were prepared by reflex method and further it is characterized and evaluated. The complex formation was estimated by FTIR analysis and drug content and drug entrapment efficiency of phytosomes was achieved to be 91.6% and 84.3% respectively. The mean diameter was found to be 854.2 nm and zeta potential 28.4 mV was found. It indicates that the in-vitro drug release of Centella asiatica were higher in comparison to the formulation complex i.e., 100% and 77.6%. The release kinetics of the optimized phytosomal formulation (F3) best fitted and the R2 value was found to be 0.9879. The anti-oxidant activity of Centella asiatica phytosomes was superior than its hydroalcoholic extract i.e., % inhibition of phytosomal formulation is 83.55 having IC50 value 1.99 and % inhibition of hydroalcoholic drug extract was 85.31 having IC50 value 2.77. In anti-ulcer activity phytosomes was found to neutralize acid more significant as compare to standard and hydroalcoholic extract of Centella asiatica. The results indicated that the prepared phytosome could be a promising candidate for effective delivery of active constituents.
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含积雪草提取物植物体抗溃疡和抗氧化活性的研制及体外评价
草药具有各种各样的活性成分,使我们能够以各种方式使用它们,但活性成分由于其强极性和低亲脂性而吸收不良,导致生物利用度低。本研究的目的是通过开发和体外评价含积雪草提取物的磷脂复合物的抗氧化和胃保护活性来提高生物利用度。采用反射法制备了积雪草磷脂复合物,并对其进行了表征和评价。FTIR分析结果表明,光复体的药物含量和包封效率分别为91.6%和84.3%。平均直径为854.2 nm, zeta电位为28.4 mV。结果表明,积雪草的体外释药率高于该制剂,分别为100%和77.6%。优化后的植体制剂(F3)的释放动力学拟合最佳,R2值为0.9879。积雪草光敏体的抗氧化活性优于水酒精提取物,即光敏体制剂的%抑制率为83.55,IC50值为1.99;水酒精药物提取物的%抑制率为85.31,IC50值为2.77。在抗溃疡活性方面,与积雪草标准提取物和积雪草水酒精提取物相比,磷脂质体对酸的中和作用更为显著。结果表明,所制备的植物体是一种有效递送活性成分的候选材料。
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