摘要
目的 本研究旨在构建人参皂苷Rg3纳米脂质体，并评估其在离体猪皮上的透皮性能，同时优化冻干工艺以确保其稳定性。方法 采用高速剪切均质技术制备人参皂苷Rg3纳米脂质体，并通过透射电镜、激光粒度仪和高效液相色谱法对其形貌、粒径、Zeta电位和包封率进行表征。利用离体猪皮模型评估纳米脂质体的透皮效率，并与人参皂苷Rg3原料药进行比较。此外，考察不同冻干工艺对纳米脂质体理化性质和包封率的影响。结果 制备的纳米脂质体呈类球形结构，平均粒径为16.0 nm，PDI为0.17，Zeta电位为-14.0 mV，包封率达到62.1%。离体猪皮透皮实验表明，人参皂苷Rg3纳米脂质体的透皮效率显著高于原料药，24 h内累积渗透量达到1069 μg/cm²，透过百分率达到94.7%。冻干工艺研究表明，液氮急速冷冻能够有效维持纳米脂质体的结构完整性和包封率，而缓慢冷冻则会导致其粒径增大、分散性变差和药物泄漏。结论 本研究成功构建了一种性能优异的人参皂苷Rg3纳米脂质体，其粒径小、分布均一、稳定性好，且能够显著提高人参皂苷Rg3的透皮效率。
关键词： 人参皂苷Rg3；纳米脂质体；透皮渗透；冻干工艺
Abstract
Objective To construct ginsenoside Rg3 nanoliposomes, evaluate their transdermal performance on excised pig skin, and optimize the freeze-drying process to ensure stability. Methods Ginsenoside Rg3 nanoliposomes were prepared using high-speed shear homogenization. Their morphology, particle size, Zeta potential, and encapsulation efficiency were characterized by transmission electron microscopy (TEM), laser particle size analysis, and high-performance liquid chromatography (HPLC). The transdermal efficiency of the nanoliposomes was assessed using an excised pig skin model and compared with that of ginsenoside Rg3 raw material. Additionally, the effects of different freeze-drying processes on the physicochemical properties and encapsulation efficiency of the nanoliposomes were investigated. Results The prepared nanoliposomes exhibited a spherical morphology with an average particle size of 16.0 nm, a PDI of 0.17, a Zeta potential of -14.0 mV, and an encapsulation efficiency of 62.1%. The ex vivo pig skin permeation study showed that the transdermal efficiency of the ginsenoside Rg3 nanoliposomes was significantly higher than that of the raw material, with a cumulative permeation amount (Qn) of 1069 μg/cm² and a permeation percentage of 94.7% within 24 h. The study on the freeze-drying process indicated that rapid freezing with liquid nitrogen effectively maintained the structural integrity and encapsulation efficiency of the nanoliposomes, whereas slow freezing led to increased particle size, poor dispersity, and drug leakage. Conclusion This study successfully prepared ginsenoside Rg3 nanoliposomes with excellent properties, including small particle size, uniform distribution, good stability, and significantly enhanced transdermal efficiency for ginsenoside Rg3.
Key words： Ginsenoside Rg3; Nanoliposomes; Transdermal permeation; Freeze-drying process
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