氧化白藜芦醇自微乳的制备、表征及美白活性的研究

doi:10.3969/j.issn.2097-2806.2025.04.007

Abstract

Abstract:

A self-microemulsifying drug delivery system （OXY-SME） was developed using Cremophor^® EL and Labrasol^® as composite emulsifiers to efficiently load oxyresveratrol （OXY）, and its formulation characteristics, stability, in vitro skin permeation, and whitening activity were evaluated. Through the pseudo-ternary phase diagram and testing the particle size and polydispersity index （PDI） of the emulsion, the formulation for the preparation of blank self-microemulsion （SME） and the optimal drug loading of OXY were determined. At the optimal drug loading of 4%, the particle size of OXY-SME was （18.69±0.29） nm, with a PDI of 0.181±0.017 and an encapsulation efficiency of 99.87%±1.50%. The emulsion droplets were spherical, and the solubility of OXY in water was increased by approximately 62 times. The relationship between emulsion type and water content of OXY-SME was clarified using water content-conductivity fitting curves and staining methods. The stability of OXY-SME under various conditions was evaluated by measuring particle size, PDI, and OXY content. The results indicate that OXY-SME exhibits good storage stability and dilution stability, and effectively delays the decrease in OXY content caused by light exposure. The effect of water content on OXY skin permeation was investigated using the abdominal skin of SD rats, and the results show that the highest cumulative skin permeation of OXY over 48 hours is observed at a water content of 70%, indicating an oil-in-water （O/W） type emulsion. The whitening activity of OXY-SME was evaluated by measuring the activity of mushroom tyrosinase and intracellular tyrosinase in B16-F10 cells, as well as melanin content. OXY-SME exhibits stronger inhibitory effects on intracellular tyrosinase activity and melanin production compared to OXY aqueous solution and kojic acid （KA） as a positive control, demonstrating that OXY-SME enhances intracellular whitening activity of OXY.

Key words: oxyresveratrol, self-microemulsion delivery system, solubility, stability, in vitro skin penetration, whitening activity

CLC Number:

TQ658

Kaiyuan Miao, Zeyao Ouyang, Xinying Zhao, Xiaojing Yang, Xinyan Chen, Zhaohua Shi. Preparation, characterization, and whitening activity research of oxyresveratrol-loaded self-microemulsion[J].China Surfactant Detergent & Cosmetics, 2025, 55(4): 453-463.

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K_m	m（Labrasol^®）:m（Cremophor^® EL）	m（油相）:m（总乳化剂）	Size/nm	PDI
2:1	1:1	1:9	217.7±4.62	0.276±0.013
2:1	1:1	2:8	17.65±0.49	0.137±0.005
2:1	1:2	1:9	14.69±0.23	0.072±0.002
2:1	1:2	2:8	23.72±0.80	0.214±0.009
2:1	1:3	1:9	15.20±0.56	0.087±0.003
2:1	1:3	2:8	51.28±1.59	0.567±0.136

K_m	m（Labrasol^®）:m（Cremophor^® EL）	m（油相）:m（总乳化剂）	Size/nm	PDI
1:1	1:2	1:9	17.00±0.22	0.137±0.04
2:1	1:2	1:9	14.69±0.16	0.072±0.02
2:1	1:2	2:8	23.72±0.68	0.214±0.09
3:1	1:2	1:9	13.87±0.22	0.123±0.02
3:1	1:2	2:8	17.38±0.56	0.164±0.04
4:1	1:2	1:9	13.28±0.13	0.195±0.08
4:1	1:2	2:8	17.15±0.25	0.159±0.02

OXY投药量/mg	粒径/nm	PDI	包封率/%	载药量/%
5	17.73±0.39	0.140±0.015	99.43±1.43	0.99±0.01
10	17.35±0.19	0.111±0.012	99.61±1.92	1.99±0.03
15	17.64±0.84	0.109±0.021	101.42±2.46	3.04±0.07
20	18.69±0.29	0.181±0.017	99.87±1.50	3.99±0.06
25	26.74±0.70	0.354±0.011	102.44±0.78	5.12±0.03
30	467.06±29.60	0.695±0.021	101.69±1.76	6.10±0.10

Preparation, characterization, and whitening activity research of oxyresveratrol-loaded self-microemulsion

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吸光度	V（L-Dopa）/μL	V（酪氨酸酶）/μL	V（样品）/μL	V（PBS）/μL	V（总体积）/μL
A	120	40		40	200
B	120			80	200
C	120	40	40		200
D	120		40	40	200