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

Abstract

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

CLC Number:

TQ658

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.

Figures/Tables 14

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References 20

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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

Preparation and evaluation of O/W microemulsions containing salicylic acid

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试剂	加入量/μL
试剂	A	B	C	D
左旋多巴	40	40	40	40
PBS	120	160	80	120
酪氨酸酶	40	0	40	0
样品溶液	0	0	40	40

方差来源	偏差平方和	自由度	均方差	F值	P值	显著性
模型	353.94	5	70.79	18.36	0.000 7	**
A：油相(肉豆蔻酸异丙酯)用量	111.13	1	111.13	28.83	0.001 0	**
B：SM(1∶1)用量	210.15	1	210.15	54.51	0.000 2	**
AB	0.072 5	1	0.072 5	0.018 8	0.894 8
A²	0.132 4	1	0.132 4	0.034 4	0.858 2
B²	29.23	1	29.23	7.58	0.028 4	*
残差	26.99	7	3.86
失拟项	20.99	3	7.00	4.67	0.085 4
误差项	5.99	4	1.50
总和	380.93	12

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水平	A	B
水平	肉豆蔻酸异丙酯用量/%	SM用量/%
-1	5	35
0	9	39
1	13	43