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日用化学工业（中英文）

日用化学工业 ›› 2021, Vol. 51 ›› Issue (10): 963-968.doi: 10.3969/j.issn.1001-1803.2021.10.006

• 开发与应用 • 上一篇    下一篇

二醇型人参皂苷W/O纳米乳的制备及其抗皮肤衰老机制研究

武子超1,叶超2,朴明贯1,*()   

  1. 1. 延边大学 药学院,吉林 延吉 133002
    2. 山东省康复医院,山东 济南 250100
  • 收稿日期:2021-02-23 修回日期:2021-09-28 出版日期:2021-10-22 发布日期:2021-10-21
  • 通讯作者: 朴明贯
  • 基金资助:
    吉林省科技发展计划项目(201603067YY)

Preparation of diol-type ginsenoside W/O nanoemulsion and research on anti-aging mechanism of skin

Wu Zichao1,Ye Chao2,Piao Mingguan1,*()   

  1. 1. College of Pharmacy, Yanbian University, Yanji, Jilin 133002, China
    2. Shandong Rehabilitation Hospital, Jinan, Shandong 250100, China
  • Received:2021-02-23 Revised:2021-09-28 Online:2021-10-22 Published:2021-10-21
  • Contact: Mingguan Piao

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摘要：

制备二醇型人参皂苷W/O纳米乳,研究其抗皮肤衰老机制。根据伪三元相图形成的纳米乳区和二醇型人参皂苷的溶解性,筛选二醇型人参皂苷纳米乳的处方;测定纳米乳的形态、粒径分布、载药量及稳定性。采用Franz扩散池研究纳米乳的体外透皮特性,HE染色法考察雄性小鼠局部给药对皮肤微观结构的影响,并考察纳米乳的抗皮肤衰老功效。二醇型人参皂苷W/O纳米乳的最佳处方为棕榈酸异丙酯（油相）、司盘80（乳化剂）、1,2-丙二醇（助乳化剂）、Km值=2、油相与混合乳化剂比例为7.5∶2.5;制得的纳米乳外观圆整、均匀,平均粒径为17 nm,粒径分布系数为0.064,二醇型人参皂苷含量为4.2 mg/mL,且物理稳定性良好。体外透皮实验结果表明,给药12 h后二醇型人参皂苷纳米乳的累计透过量为1.640 7 mg/cm2,皮肤滞留量为0.018 4 mg/cm2,分别为二醇型水溶液的2.832 2倍和1.179 5倍;HE染色实验发现,使用人参皂苷纳米乳后结构基本完整,无病理学病变,真皮胶原纤维致密丰富,多排列成束。动物实验结果表明,二醇型人参皂苷纳米乳高、中、低剂量组的羟脯胺酸、Ⅰ型胶原、Ⅲ型胶原、基质金属蛋白酶抑制剂1（TIMP-1）、基质金属蛋白酶抑制剂2（TIMP-2）含量均显著大于空白组和二醇型人参皂苷水溶液组,基质金属蛋白酶1（MMP-1）含量显著小于空白组和二醇型人参皂苷水溶液组。制备的人参皂苷纳米乳稳定性好,透皮性能优良,能通过抑制皮肤内胶原蛋白分解,提高皮肤中胶原蛋白含量达到抗皮肤衰老功效。

关键词: 二醇型人参皂苷, W/O纳米乳, 皮肤滞留量, 抗皮肤衰老

Abstract:

The diol-type ginsenoside W/O nanoemulsion was prepared and its anti-aging mechanism of skin was studied. According to the solubility of the diol-type ginsenoside and the pseudo-ternary phase diagram, we investigated the nanoemulsion prescription, and determined the nanoemulsion morphology, particle size distribution, drug loading and stability. The Franz diffusion cell was used to study the in vitro transdermal properties of the nanoemulsion, and the effect of local administration of the nanoemulsion on male mice skin microstructure was investigated by HE staining method. And the anti-aging effects of nanoemulsion was investigated as well. The best prescription for diol-type ginsenoside W/O nanoemulsion is isopropyl palmitate as oil phase, Span 80 as emulsifier, 1, 2-propylene glycol as co-emulsifier, and Km value=2. The ratio of oil phase to mixed emulsifier is 7.5∶2.5. The nanoemulsion has a round and uniform appearance, the average particle size is 17 nm, the particle size distribution value is 0.064, and the glycol-type ginsenoside content is 4.2 mg/mL. The physical stability is good. The results of in vitro transdermal experiments show that the cumulative permeation of the ginsenoside nanoemulsion is 1.640 7 mg/cm 2 after 12 h of transdermal administration, which is 2.832 2 times that of the cumulative permeation of 12 h in aqueous solution. The skin retention is 0.018 4 mg/cm2, which is 1.179 5 times that of the skin retention of the aqueous solution. The HE staining experiment is found that the structure of the epidermal structure is basically intact without pathological changes after using the ginsenoside nanoemulsion. The dermal collagen fibers are dense and abundant, mostly arrange in bundles. The results of animal experiments show that hydroxyproline, type I collagen, type III collagen, matrix metalloproteinase inhibitor 1 （TIMP-1）, and matrix metalloproteinase inhibitor 2 （TIMP-2） content are significantly higher than the blank group and the ginsenoside aqueous solution group, and the contents of matrix metalloproteinase 1 （MMP-1） are significantly lower than those in the blank group and the aqueous solution group. The prepared ginsenoside nanoemulsion has good stability and excellent transdermal performance, and can achieve anti-aging effects by inhibiting the decomposition of collagen and increasing the collagen content in the skin.

Key words: diol type ginsenoside, W/O nanoemulsion, skin retention, anti-skin aging

中图分类号: 

  • TQ658