人参皂苷Rh2纳米脂质体制备与评价

Preparation and Evaluation of Ginsenoside Rh2 Nanoliposomes

摘要: 目的：本研究旨在构建人参皂苷Rh2纳米脂质体，并对其理化性质、皮肤渗透性和冷冻干燥条件进行系统评价，为开发人参皂苷Rh2透皮递送系统提供科学依据。方法：采用均质法制备人参皂苷Rh2纳米脂质体，并利用透射电镜、激光粒度仪等手段对其进行形态观察、粒径分布、包封率、Zeta电位等理化性质的表征。通过离体猪皮肤渗透实验，测定人参皂苷Rh2纳米脂质体的皮肤渗透性能，并与原料药进行对比，评估其透皮递送效果。此外，还研究了冻干工艺对人参皂苷Rh2纳米脂质体稳定性的影响。结果：所制备的纳米脂质体呈类球形结构，粒径分布均匀，平均粒径为15.6 nm，PDI为0.07，Zeta电位为−16.8 mV，包封率达66.2%。离体猪皮肤渗透实验结果表明，人参皂苷Rh2纳米脂质体展现出优异的透皮性能，其透皮百分率达到90.5%，显著高于人参皂苷Rh2原料药(1.1%)。稳定性实验结果表明，液氮急速冷冻(−196℃)是保护人参皂苷Rh2脂质体结构完整性和包封效率的最优策略，而缓慢冷冻会导致脂质体结构破坏和药物泄露。结论：人参皂苷Rh2纳米脂质体是一种高效皮肤递送系统，能够显著提高人参皂苷Rh2的皮肤渗透性，具有化妆品与经皮给药制剂的开发潜力。

Abstract: Objective: This study aimed to construct ginsenoside Rh2 nanoliposomes and to systematically evaluate their physicochemical properties, skin permeability, and freeze-drying conditions, so as to provide a scientific basis for the development of a ginsenoside Rh2 transdermal delivery system. Methods: Ginsenoside Rh2 nanoliposomes were prepared by the homogenization method. Their physicochemical properties, including morphology, particle size distribution, encapsulation efficiency, and Zeta potential, were characterized using Transmission Electron Microscopy (TEM) and a laser particle size analyzer. The skin permeability of the nanoliposomes was determined through ex vivo pig skin permeation experiments and compared with that of the raw drug to evaluate the transdermal delivery effect. Furthermore, the effect of the freeze-drying process on the stability of the ginsenoside Rh2 nanoliposomes was investigated. Results: The prepared nanoliposomes exhibited a spherical-like structure with a uniform particle size distribution. The average particle size was 15.6 nm, the PDI was 0.07, the Zeta potential was −16.8 mV, and the encapsulation efficiency reached 66.2%. The ex vivo pig skin permeation experiment showed that the ginsenoside Rh2 nanoliposomes exhibited excellent transdermal performance, with a penetration percentage of 90.5%, significantly higher than that of the ginsenoside Rh2 raw material (1.1%). The stability experiment indicated that rapid freezing with liquid nitrogen (−196˚C) was the optimal strategy to protect the structural integrity and encapsulation efficiency of the liposomes, whereas slow freezing led to structural damage and drug leakage. Conclusion: Ginsenoside Rh2 nanoliposomes represent an efficient skin delivery system that can significantly enhance the skin permeability of ginsenoside Rh2, demonstrating potential for development in cosmetics and transdermal drug delivery formulations.