O/W型水杨酸微乳的制备与质量评价

doi:10.3969/j.issn.2097-2806.2026.02.005

摘要/Abstract

摘要：

文章通过溶解度分析、伪三元相图优化及星点设计-响应面法，制备了水杨酸微乳，并对其进行了质量评价。采用肉豆蔻酸异丙酯作为油相，吐温80与聚乙二醇400（质量比为1∶1）作为混合表面活性剂体系，优化了微乳配方。实验结果表明，最佳配方为油相用量5%，表面活性剂混合物用量42.7%，最大载药量达到48.303 mg/g。制备的微乳为透明澄清的O/W型液体，粒径为（7.66 ± 0.31）nm，多分散系数为0.11 ± 0.04，具有良好的热稳定性和冻融稳定性。体外释放实验显示，水杨酸微乳在不同介质中均具有缓释效果，48 h累积释放率接近82%~96%，显著优于游离水杨酸。酪氨酸酶抑制实验表明，水杨酸微乳显著提升了酪氨酸酶抑制效果，含量达0.5%及以上时，抑制率超过95%。研究结果表明，优化后的微乳配方具有良好的载药能力、稳定性及缓释特性，能够有效提升水杨酸的药效，可作为潜在的药物递送载体，为水杨酸的临床应用提供新的技术支持。

关键词: 水杨酸, 微乳, 紫外分光光度法, 伪三元相图, 星点设计-响应面法

Abstract:

The O/W microemulsions containing salicylic acid were prepared and evaluated. Isopropyl myristate was used as the oil phase and a mixture of Tween 80 and polyethylene glycol 400（1 : 1）was used as the mixed surfactants. The microemulsion formulation was optimized by solubility analysis, pseudo-ternary phase diagram construction, and central composite design-response surface methodology. The results showed that, the optimized formulation, consisting of 5% oil phase and 42.7% surfactant mixture, achieved a maximum drug-loading capacity of 48.303 mg/g. The microemulsion thus prepared was a transparent, clear O/W liquid with particle size of（7.66± 0.31）nm and polydispersity index of 0.11±0.04, demonstrating excellent thermal and freeze-thaw stabilities. In vitro release experiments showed that the microemulsion exhibited sustained release of salicylic acid in different media, with cumulative release rates approaching 82% to 96% over 48 hours, which was significantly higher than those of free salicylic acid. In addition, in vitro tyrosinase inhibition assays indicated that the microemulsion enhanced the bioavailability of salicylic acid, achieving inhibition rate of over 95% when the salicylic acid content was 0.5% or more. In conclusion, the optimized microemulsion formulation had superior drug-loading capacity, stability, and sustained-release characteristics, effectively improving the therapeutic efficacy of salicylic acid. This microemulsion system was proposed as a potential drug delivery carrier, which might offer new technical support for the clinical application of salicylic acid.

Key words: salicylic acid, microemulsion, ultraviolet spectrophotometry, pseudo-ternary phase diagram, central composite design-response surface method

中图分类号:

TQ658

赵洋, 王艳, 唐文杰, 任硕晗, 张桂红, 李疆改. O/W型水杨酸微乳的制备与质量评价[J]. 日用化学工业（中英文）, 2026, 56(2): 176-184.

Yang Zhao, Yan Wang, Wenjie Tang, Shuohan Ren, Guihong Zhang, Jianggai Li. Preparation and evaluation of O/W microemulsions containing salicylic acid[J]. China Surfactant Detergent & Cosmetics, 2026, 56(2): 176-184.

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微乳等级划分	乳化时间/min	微乳外观
A	<1	微蓝色乳光澄清
B	<1	稍浑浊，泛蓝色乳光
C	1~3	浑浊，蓝白色液体
D	3~5	呈灰白色，略带油状液体
E	>5	乳化失败，油相分层明显

序号	样品加入量/mg	标品加入量/mg	测得总和/mg	理论总和/mg	回收率/%	平均回收率/%	RSD/%
1	25.050	20.040	46.270	45.090	102.616	102.17	0.38
2	25.050	20.040	45.963	45.090	101.936
3	25.050	20.040	45.978	45.090	101.969
4	25.050	25.050	49.269	50.100	98.342	98.50	0.14
5	25.050	25.050	49.409	50.100	98.621
6	25.050	25.050	49.363	50.100	98.529
7	25.050	30.060	53.683	55.110	97.410	97.33	0.14
8	25.050	30.060	53.552	55.110	97.172
9	25.050	30.060	53.684	55.110	97.412

分类	溶媒	溶解度/(mg/mL)
油相	肉豆蔻酸异丙酯	44.610 ± 0.003
	葡萄籽油	28.644 ± 0.039
	小麦胚芽油	17.697 ± 0.083
表面活性剂	吐温20	26.974 ± 0.224
	吐温80	32.010 ± 0.006
	辛酸癸酸聚乙二醇甘油酯	38.028 ± 0.085
助表面活性剂	二乙二醇单乙基醚	466.699 ± 1.855
	聚乙二醇400	73.094 ± 0.022
	甘油	19.496 ± 0.041

油相/表面活性剂/助表面活性剂	乳化情况评价	微乳稳定性
肉豆蔻酸异丙酯/辛酸癸酸聚乙二醇甘油酯/二乙二醇单乙基醚	C	分层
葡萄籽油/辛酸癸酸聚乙二醇甘油酯/二乙二醇单乙基醚	D	分层
肉豆蔻酸异丙酯/吐温80/二乙二醇单乙基醚	D	分层
葡萄籽油/吐温80/二乙二醇单乙基醚	D	分层
肉豆蔻酸异丙酯/辛酸癸酸聚乙二醇甘油酯/聚乙二醇400	E	分层
葡萄籽油/吐温80/聚乙二醇400	D	分层
肉豆蔻酸异丙酯/吐温80/聚乙二醇400	B	不分层
葡萄籽油/辛酸癸酸聚乙二醇甘油酯/聚乙二醇400	E	分层

组别	肉豆蔻酸异丙酯用量	SM用量	最大载药量/（mg/g）
1	-1	-1	33.851
2	0	0	40.712
3	0	0	42.440
4	0	-1	33.615
5	-1	1	48.070
6	1	0	35.007
7	1	-1	27.094
8	0	0	39.293
9	1	1	40.774
10	0	0	39.656
11	0	0	40.368
12	-1	0	46.777
13	0	1	41.225