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新型传递体与天然抗氧化剂白藜芦醇的制备及评价。

Preparation and Evaluation of Novel Transfersomes Combined with the Natural Antioxidant Resveratrol.

机构信息

Department of Cosmetic Science, Providence University, Taichung 43301, Taiwan.

Department of Applied Chemistry, Providence University, Taichung 43301, Taiwan.

出版信息

Molecules. 2019 Feb 8;24(3):600. doi: 10.3390/molecules24030600.

Abstract

Resveratrol (-3,5,4'-trihydroxystibene, RSV) is a kind of polyphenol which has anti-inflammatory, antioxidant, anti-allergy, and anti-cancer properties, as well as being a scavenger of free radicals and preventing cardiovascular diseases. However, it is quite unstable in light, heat, and other conditions, and decays easily due to environmental factors. For these reasons, this study used a new type of carrier, transfersome, to encapsulate RSV. Transfersome consists of phosphatidyl choline (PC) from a liposomal system and non-ionic edge activators (EA). EA are an important ingredient in the formulation of transfersome; they can enhance the flexibility of the lipid bimolecular membrane of transfersome. Due to its ultradeformability, it also allows drugs to penetrate the skin, even through the stratum corneum. We hope that this new encapsulation technique will improve the stability and enhance the permeability of RSV. Concluding all the tested parameters, the best production condition was 5% PC/EA (3:1) and 5% ethanol in distilled water, with an ultrasonic bath and stirring at 500 rpm, followed by high pressure homogenization. The optimal particle size was 40.13 ± 0.51 nm and the entrapment efficiency (EE) was 59.93 ± 0.99%. The results of antioxidant activity analysis showed that transfersomes were comparable to the RSV group (unencapsulated). During in vitro transdermal delivery analysis, after 6 h, D1-20(W) increased 27.59% by accumulation. Cell viability assay showed that the cytotoxicity of D3-80(W) was reduced by 34.45% compared with the same concentration of RSV. Therefore, we successfully prepared RSV transfersomes and also improved the stability, solubility, and safety of RSV.

摘要

白藜芦醇(-3,5,4'-三羟基二苯乙烯, RSV)是一种多酚,具有抗炎、抗氧化、抗过敏和抗癌特性,同时也是自由基清除剂,可预防心血管疾病。然而,它在光、热和其他条件下极不稳定,容易因环境因素而降解。出于这些原因,本研究使用了一种新型载体——转胞体来包裹 RSV。转胞体由脂质体系统中的磷脂酰胆碱(PC)和非离子型边缘活性剂(EA)组成。EA 是转胞体配方中的重要成分;它们可以增强转胞体双分子脂质膜的柔韧性。由于其超高的变形能力,它还可以使药物穿透皮肤,甚至穿过角质层。我们希望这种新的封装技术将提高 RSV 的稳定性并增强其渗透性。综合所有测试参数,最佳生产条件为 5% PC/EA(3:1)和 5%乙醇在蒸馏水中,采用超声浴和 500 rpm 的搅拌,然后进行高压匀浆。最佳粒径为 40.13±0.51nm,包封率(EE)为 59.93±0.99%。抗氧化活性分析结果表明,转胞体与 RSV 组(未包裹)相当。在体外透皮传递分析中,6 小时后,D1-20(W) 通过累积增加了 27.59%。细胞活力测定表明,与相同浓度的 RSV 相比,D3-80(W) 的细胞毒性降低了 34.45%。因此,我们成功制备了 RSV 转胞体,同时提高了 RSV 的稳定性、溶解度和安全性。

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