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含有脂质体的玫瑰茄萼片提取物制剂,具有增强的抗氧化活性、改善的皮肤渗透性和降低的皮肤毒性。

Liposome-containing Hibiscus sabdariffa calyx extract formulations with increased antioxidant activity, improved dermal penetration and reduced dermal toxicity.

作者信息

Pinsuwan Sirirat, Amnuaikit Thanaporn, Ungphaiboon Suwipa, Itharat Arunporn

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Songkhla, Thailand.

出版信息

J Med Assoc Thai. 2010 Dec;93 Suppl 7:S216-26.

Abstract

Hibiscus sabdariffa Linn, or Roselle, is a medicinal plant used extensively in traditional Thai medicine since ancient times. The extracts of Roselle calyces possess antioxidant activity and have potential for development as active ingredients in cosmetic products. However the limitations of using Roselle extracts in cosmetics are its low skin permeation and dermal irritation. Liposome technology is an obvious approach that might overcome these problems. Liposome formulations of standardized Roselle extracts were developed with various lipid components. The formulation showing the highest entrapment efficiency was selected for stability, skin permeation and dermal irritability studies. The liposome formulation with the highest entrapment efficiency (83%) and smalôlest particle size (332 mm) was formulated with phosphatidylcholine from soybean (SPC): Tween 80: deoxycholic acid (DA); 84:16:2.5 weight ratio, total lipid of 200 g/mL and 10% w/v Roselle extract in final liposomal preparation. This liposome formulation was found to be stable after storage at 4 degrees C, protected from light, for 2 months. The in vitro skin permeation studies, using freshly excised pig skin and modified Franz-diffusion cells, showed that the liposome formulation was able to considerably increased the rate of permeation of active compounds in Roselle extracts compared to the Roselle extract solution. The in vivo dermal irritability testing on rabbit skin showed that the liposome formulation dramatically decreased skin irritability compared to the unformulated extract. These results showed that the liposomes containing Roselle extracts had good stability, high entrapment efficacy, increased skin permeation and low skin irritation.

摘要

玫瑰茄,即洛神花,是一种药用植物,自古以来就在泰国传统医学中广泛使用。玫瑰茄花萼提取物具有抗氧化活性,有潜力开发成为化妆品中的活性成分。然而,在化妆品中使用玫瑰茄提取物的局限性在于其皮肤渗透率低和有皮肤刺激性。脂质体技术显然是一种可能克服这些问题的方法。用各种脂质成分开发了标准化玫瑰茄提取物的脂质体制剂。选择包封率最高的制剂进行稳定性、皮肤渗透性和皮肤刺激性研究。包封率最高(83%)且粒径最小(332毫米)的脂质体制剂由大豆磷脂酰胆碱(SPC)、吐温80、脱氧胆酸(DA)按84:16:2.5的重量比配制而成,最终脂质体制剂中总脂质为200克/毫升,玫瑰茄提取物为10%(w/v)。发现这种脂质体制剂在4℃避光储存2个月后是稳定的。使用新鲜切除的猪皮和改良的Franz扩散池进行的体外皮肤渗透研究表明,与玫瑰茄提取物溶液相比,脂质体制剂能够显著提高玫瑰茄提取物中活性化合物的渗透速率。对兔皮进行的体内皮肤刺激性测试表明,与未配制的提取物相比,脂质体制剂显著降低了皮肤刺激性。这些结果表明,含有玫瑰茄提取物的脂质体具有良好的稳定性、高包封率、增加的皮肤渗透性和低皮肤刺激性。

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