用于改善透明质酸透皮性能的阳离子脂质体递送系统的构建与评价

doi:10.3969/j.issn.2097-2806.2026.04.005

摘要/Abstract

摘要：

针对大分子透明质酸（HA）经皮渗透效率低的问题开发了一种基于十八烷基三甲基氯化铵（OTAC）的阳离子脂质体（OTAC-L）递送系统，该系统通过静电作用实现了对HA的高效包载（包封率为89%），并显著增强了其经皮渗透能力。首先通过粒径、Zeta电位、包封率的测定、荧光探针对膜性质的分析以及鸡胚实验进行OTAC加入量的优化，成功制备出粒径为（90.42±1.92） nm，多分散指数为0.23±0.02的阳离子透明质酸脂质体（OTAC-HA-L）。透射电子显微镜观察证实脂质体为形态规整的球形结构，低场核磁共振与等温量热滴定分别通过研究脂质体水分子运动状态的变化和与HA结合过程的热力学参数，验证了HA与阳离子脂质体之间的高效结合。傅里叶变换红外光谱分析揭示了HA的特征吸收峰变化，证实其被成功包载，并与脂质体间存在静电相互作用。体外渗透实验表明，OTAC-HA-L的透皮性能显著提升，12 h累积透过率达到15.3%，分别为普通脂质体和HA水溶液的1.91倍和2.56倍。且其在常温、高温和低温条件下均表现出良好稳定性，为HA在皮肤护理领域的深层递送提供了一种具有重要应用前景的解决方案。

关键词: 透明质酸, 阳离子脂质体, 经皮渗透, 包封率

Abstract:

In this study, we developed a cationic liposome （OTAC-L） delivery system based on octadecyltrimethylammonium chloride （OTAC） to enhance the low percutaneous permeability of hyaluronic acid. OTAC-HA-L was successfully prepared, showing a particle size of （90.42±1.92）nm and a polydispersity index of 0.23±0.02. This was achieved through measurements of particle size, Zeta potential, and entrapment efficiency, as well as analysis film properties using a fluorescence probe and optimizing the OTAC amount in chicken embryo experiments. Transmission electron microscopy （TEM） confirmed that the liposomes had a regular spherical shape. Low-field NMR and isothermal calorimetry were employed to investigate the molecular movement of water and the thermodynamic parameters of the HA binding process, respectively, confirming the effective binding between HA and cationic liposomes. Fourier transform infrared spectroscopy （FT-IR） identified the characteristic absorption peak of HA, confirming successful loading of HA and interaction with the liposomes. In vitro permeation tests showed that OTAC-HA-L’s permeation performance was significantly improved, with a cumulative permeation rate of 15% at 12 hours, which was 1.91 and 2.56 times higher than that of standard liposomes and aqueous HA, respectively. Additionally, the system demonstrated good stability under normal-, high-, and low-temperature conditions, making it a promising approach for deep HA delivery in skin care.

Key words: hyaluronic acid, cationic liposomes, percutaneous penetration, encapsulation efficiency

中图分类号:

TQ658

王宇, 任爽, 杨素珍, 韩婷婷, 姬迎迎, 张子嘉, 张婉萍. 用于改善透明质酸透皮性能的阳离子脂质体递送系统的构建与评价[J]. 日用化学工业（中英文）, 2026, 56(4): 449-462.

Yu Wang, Shuang Ren, Suzhen Yang, Tingting Han, Yingying Ji, Zijia Zhang, Wanping Zhang. Construction of a cationic liposomal system for enhanced transdermal delivery of hyaluronic acid[J]. China Surfactant Detergent & Cosmetics, 2026, 56(4): 449-462.

图/表 12

参考文献 21

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w_OTAC/%	Reaction situation	Chicken embryo 1	Chicken embryo 2	Chicken embryo 3	ES
0	Bleeding	0	0	0	0
	Coagulation	0	0	0
	Vascular dissolution	0	0	0
0.1	Bleeding	0	0	0	0
	Coagulation	0	0	0
	Vascular dissolution	0	0	0
0.5	Bleeding	1	1	0	0.67
	Coagulation	0	0	0
	Vascular dissolution	0	0	0
1	Bleeding	1	1	1	1.67
	Coagulation	0	0	1
	Vascular dissolution	0	0	1
2	Bleeding	2	2	2	2.33
	Coagulation	1	0	0
	Vascular dissolution	0	0	0