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人参皂苷Rb1的黑色素生成抑制作用及经皮制剂

The melanogenesis-inhibitory effect and the percutaneous formulation of ginsenoside Rb1.

作者信息

Wang Lin, Lu Ai-Ping, Yu Zhi-Ling, Wong Ricky N S, Bian Zhao-Xiang, Kwok Hoi-Hin, Yue Patrick Ying-Kit, Zhou Li-Min, Chen HuBiao, Xu Min, Yang Zhijun

机构信息

School of Chinese Medicine, Hong Kong Baptist University, 7 Baptist University Road, Kowlong Tong, Kowloon, Hong Kong, China.

出版信息

AAPS PharmSciTech. 2014 Oct;15(5):1252-62. doi: 10.1208/s12249-014-0138-3. Epub 2014 Jun 4.

Abstract

Ginsenoside Rb1 (Rb1) is the most predominant ginsenoside isolated from the roots of ginseng (Panax ginseng C. A. Meyer). This compound is active in various human biological pathways that are involved in human collagen synthesis and inhibition of cell apoptosis. In this study, the skin-whitening effects of Rb1 were investigated in B16 melanoma cells. Our results showed that Rb1 inhibited melanogenesis in α-melanocyte-stimulating hormone (α-MSH)-stimulated B16 cells in a dose-dependent manner, which collectively indicated that Rb1 may have skin-whitening effects and may be formulated into skin-whitening products for skin care. Accordingly, a ginsenoside collagen transdermal patch was developed as a vehicle to topically deliver Rb1 into pig skin. The percutaneous permeation, retention within skin, and release in vitro of Rb1 from seven transdermal patch formulas were studied. It was determined that the best formula for ginsenoside collagen transdermal patch is made of protein collagen hydrolysate powder (PCHP) 2.0% (w/w), methyl cellulose (MC) 0.5% (w/w), polyethyleneglycol 6000 (PEG6000) 0.5% (w/w), ginsenoside 0.036% (w/w), azone 0.4% (v/w), menthol 0.20% (w/w), and water.

摘要

人参皂苷Rb1(Rb1)是从人参(Panax ginseng C. A. Meyer)根中分离出的最主要的人参皂苷。该化合物在参与人体胶原蛋白合成和抑制细胞凋亡的各种人体生物途径中具有活性。在本研究中,研究了Rb1在B16黑色素瘤细胞中的美白效果。我们的结果表明,Rb1以剂量依赖性方式抑制α-黑素细胞刺激激素(α-MSH)刺激的B16细胞中的黑色素生成,这共同表明Rb1可能具有美白效果,并且可以配制成用于皮肤护理的美白产品。因此,开发了一种人参皂苷胶原蛋白透皮贴剂作为将Rb1局部递送至猪皮肤的载体。研究了七种透皮贴剂配方中Rb1的经皮渗透、在皮肤中的保留以及体外释放情况。确定人参皂苷胶原蛋白透皮贴剂的最佳配方由2.0%(w/w)的蛋白质胶原蛋白水解物粉末(PCHP)、0.5%(w/w)的甲基纤维素(MC)、0.5%(w/w)的聚乙二醇6000(PEG6000)、0.036%(w/w)的人参皂苷、0.4%(v/w)的氮酮以及0.20%(w/w)的薄荷醇和水制成。

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