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Anti-inflammatory activity of liposomes of Asparagus racemosus root extracts prepared by various methods

机译:用多种方法制备的芦笋根提取物脂质体的抗炎活性

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Asparagus racemosus root extracts (AR) have been reported to possess a variety of pharmacological properties. The aim of the present study was to develop liposomes of AR and to assess their physicochemical characteristics and anti-inflammatory activity in the monocytic leukemia cell line THP-1. Liposomes containing various ratios of AR to lipid and a phosphatidylcholine to cholesterol molar ratio of 7:3 were prepared by thin-film hydration (TF), reverse-phase evaporation (REV) and polyol dilution (PD). The results showed that AR liposomes prepared by TF had a multilamellar structure and a large size, whereas those prepared by REV and PD were oligolamellar in structure, and of a smaller size. The particle sizes and zeta potentials of the liposomes ranged from 196.5 to 456.6 nm and from -4.34 to -18.94 mV, respectively. The AR to lipid ratio was shown to have no significant influence on particle size, while the zeta potential generally increased with increasing AR to lipid ratio. The highest entrapment efficiency values were detected in liposomes with an AR to lipid ratio of 1:5, and for liposomes prepared by TF, REV and PD methods, the entrapment efficiencies were 55.71 +/- 2.04, 56.21 +/- 3.59 and 67.68 +/- 1.37%, respectively. AR was found to exert no toxicity on THP-1 cells. The maximum anti-inflammatory activities of AR and AR liposomes, evaluated in terms of the percentage inhibition of tumor necrosis factor- in THP-1 cells, were similar to 52% at a concentration of 1 mu g/ml. It can be concluded from the present study that AR liposomes have the potential to be used a formulation for topical and/or transdermal drug delivery to provide anti-inflammatory activity.
机译:据报道,芦笋根提取物(AR)具有多种药理特性。本研究的目的是开发AR脂质体,并评估其在单核细胞白血病细胞系THP-1中的理化特性和抗炎活性。通过薄膜水合(TF),反相蒸发(REV)和多元醇稀释(PD)制备了含有各种比例的AR与脂质和磷脂酰胆碱与胆固醇摩尔比为7:3的脂质体。结果表明,由TF制备的AR脂质体具有多层结构且尺寸大,而由REV和PD制备的AR脂质体结构低聚且尺寸较小。脂质体的粒径和ζ电势分别在196.5至456.6nm和-4.34至-18.94mV的范围内。已显示,AR与脂质的比率对粒度没有显着影响,而Zeta电位通常随AR与脂质的比率增加而增加。在AR与脂质比率为1:5的脂质体中检测到最高的包封效率值,对于通过TF,REV和PD方法制备的脂质体,包封率为55.71 +/- 2.04、56.21 +/- 3.59和67.68 + -分别为1.37%。发现AR对THP-1细胞没有毒性。以THP-1细胞中肿瘤坏死因子抑制百分比的形式评估,AR和AR脂质体的最大抗炎活性在1μg / ml的浓度下接近52%。从本研究可以得出结论,AR脂质体具有被用于局部和/或透皮药物递送的制剂以提供抗炎活性的潜力。

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