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首页> 美国卫生研究院文献>Molecules >Preparation Characterization and Antioxidant Activity Evaluation of Liposomes Containing Water-Soluble Hydroxytyrosol from Olive
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Preparation Characterization and Antioxidant Activity Evaluation of Liposomes Containing Water-Soluble Hydroxytyrosol from Olive

机译：橄榄中水溶性羟基酪醇脂质体的制备表征及抗氧化活性评价

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摘要

Due to the multiple hydroxyl groups in its structure, hydroxytyrosol (HT) is very sensitive to air and light and has very strong instability and hydrophilicity that affect its biological activity. This study attempted to prepare liposomes containing water-soluble HT to improve the bioavailability and biocompatibility of the target drug. The preparation process factors (temperature, mass ratio of phospholipid (PL) and cholesterol (CH), Tween-80 volume, HT mass) were studied and response surface methodology (RSM) was applied to optimize the conditions. The results demonstrated that by using a temperature of 63 °C, mass ratio of PL and CH 4.5:1, HT mass 5 mg and Tween-80 volume of 6 mL, HT liposomes with an encapsulation efficiency (EE) of 45.08% were prepared. It was found that the particle sizes of the HT liposomes were well distributed in the range of 100–400 nm. Compared to free HT, prepared HT liposomes had better stability and a distinct slow release effect in vitro. Besides, HT liposomes presented better DPPH radical scavenging activity than free HT, which could be due to the fact that HT was encapsulated fully inside the liposomes. In addition, the encapsulation mechanism of HT was evaluated. In summary, the results indicated that HT liposome could enhance the antioxidant activity and was a promising formulation for prolonging the biological activity time of the target drug.
机译：由于其结构中有多个羟基，羟基酪醇（HT）对空气和光线非常敏感，并且具有非常强的不稳定性和亲水性，从而影响其生物学活性。这项研究试图制备含有水溶性HT的脂质体，以提高目标药物的生物利用度和生物相容性。研究了制备工艺因素（温度，磷脂（PL）与胆固醇（CH）的质量比，吐温80体积，HT质量），并采用响应面法（RSM）优化了工艺条件。结果表明，通过使用63°C的温度，PL和CH的质量比为4.5：1，HT质量为5 mg，Tween-80体积为6 mL，制备了包封效率（EE）为45.08％的HT脂质体。 。研究发现，HT脂质体的粒径分布在100-400 nm范围内。与游离HT相比，制备的HT脂质体在体外具有更好的稳定性和明显的缓释作用。此外，HT脂质体表现出比游离HT更好的DPPH自由基清除活性，这可能是由于HT完全包裹在脂质体内。另外，评估了HT的包囊机理。总之，结果表明HT脂质体可以增强抗氧化活性，并且是延长靶药物的生物活性时间的有希望的制剂。

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