阿魏酸纳米醇质体的制备、表征及体外经皮吸收研究

doi:10.3969/j.issn.2097-2806.2023.11.007

摘要/Abstract

摘要：

研究了微射流技术制备的阿魏酸纳米醇质体经皮递送和抗氧化性能。首先，采用响应面法研究了卵磷脂、边缘活化剂（蔗糖棕榈酸酯、吐温-80）对阿魏酸纳米醇质体包封率的影响，优化得到：卵磷脂、蔗糖棕榈酸酯与吐温-80为0.68%:0.51%:0.25%（w/%）时，所制备的阿魏酸纳米醇质体粒径小且分布均匀（（104.5±0.7） nm），PDI为0.05±0.01，包封率高（88.8%±2.6%），稳定性高（25 ℃稳定存放60天）。其次，采用DPPH自由基清除实验和Franz扩散池体外透皮实验分别评价了阿魏酸纳米醇质体的抗氧化性能和经皮递送性能，阿魏酸纳米醇质体的IC₅₀值为8.7 μg/mL，抗氧化活性略高于阿魏酸丙二醇水溶液（IC₅₀值为11.7 μg/mL）；阿魏酸纳米醇质体皮肤滞留量和累积透过量分别为（18.2±3.5） μg/cm²和（25.3±3.2） μg/cm²，分别是阿魏酸丙二醇水溶液的1.2倍和1.4倍。研究发现，制备的阿魏酸纳米醇质体粒径均一、包封率高、稳定性好且抗氧化性高、经皮吸收性能好，有望用于酚酸类天然活性物经皮递送系统，及其抗氧化、抗衰老、美白等功效化妆品。

关键词: 阿魏酸, 纳米醇质体, 微射流, 抗氧化, 经皮吸收

Abstract:

The transdermal delivery and antioxidant of ferulic acid nanoethosomes prepared by microfluidization were studied. Firstly, the effects of edge-activators （Tween-80, and sucrose palmitate） and lecithin on the encapsulation efficiency of ferulic acid nanoethosomes were investigated by the response surface method. When lecithin, sucrose palmitate and Tween-80 are optimized at the ratio of 0.68%:0.51%:0.25% （w/%）, the ferulic acid nanoethosomes demonstrate better characteristics of small particle size of （104.5±0.7） nm, uniform particle size distribution with PDI of 0.05±0.01, high encapsulation efficiency of 88.8%±2.6%, and high storage stability for 60 days at 25 ℃. Secondly, the antioxidant ability and the skin penetration property of ferulic acid and its nanoethosomes were evaluated by DPPH free radical scavenging tests and in vitro transdermal assays using Franz diffusion cells, respectively. The IC₅₀ values of ferulic acid and its nanoethosomes are 8.7 and 11.7 μg/mL, respectively, indicating that the ferulic acid nanoethosomes exhibite enhanced antioxidant activity. It is found that the nanoethosomes have better skin permeability and their skin adsorption amount and accumulated permeation amount of the nanoethosomes are （18.2±3.5） μg/cm² and （25.3±3.2） μg/cm², which are 1.2 times and 1.4 times higher than that of the ferulic acid propylene glycol solution, respectively. The prepared ferulic acid nanoethosomes have the advantages of uniform particle size, high encapsulation efficiency and storage stability, enhanced antioxidant ability and skin permeability, and can be extended to the preparation of other phenolic acid nanoethosomes and applied as transdermal carriers for antioxidant, anti-aging, and whitening cosmetics.

Key words: ferulic acid, nanoethosomes, microfluidization, antioxidant, skin penetration

中图分类号:

TQ658

邓梦洁, 易国斌, 吕冉, 柳亚锋, 叶大威, 陈佳志. 阿魏酸纳米醇质体的制备、表征及体外经皮吸收研究[J]. 日用化学工业（中英文）, 2023, 53(11): 1285-1292.

Deng Mengjie, Yi Guobin, Lv Ran, Liu Yafeng, Ye Dawei, Chen Jiazhi. Ferulic acid nanoethosomes: preparation, characterization, and performance of skin penetration in vitro[J]. China Surfactant Detergent & Cosmetics, 2023, 53(11): 1285-1292.

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参考文献 18

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水平	因素
水平	A（卵磷脂含量/%）	B（蔗糖棕榈酸酯含量/%）	C（吐温-80含量/%）
-1	0.1	0.4	0.1
0	0.5	0.5	0.25
1	0.9	0.6	0.4

方差来源	平方和	自由度	均方	F值	P值
模型	4 634.75	9	514.97	80.03	<0.000 1
A	2 489.36	1	2 489.36	386.87	<0.000 1
B	4.40	1	4.40	0.68	0.44
C	0.11	1	0.11	0.02	0.90
AB	0.18	1	0.18	0.03	0.87
AC	37.52	1	37.52	5.83	0.05
BC	48.72	1	48.72	7.57	0.03
A²	1 706.26	1	1 706.26	265.17	<0.000 1
B²	19.52	1	19.52	3.03	0.13
C²	220.89	1	220.89	34.33	0.00
残差	45.04	7	6.43
失拟	38.01	3	12.67	7.21	0.04
纯误差	7.03	4	1.76
总和	4 679.79	16
R²=0.990 4，R²_Adj=0.978 0