人参皂苷是人参的主要生物活性化合物。人参总皂苷(GS)含有多种皂苷单体,具有有效的抗光老化活性和改善皮肤屏障功能。为了提高GS的透皮吸收效率,将GS脂质体(GSL)和GS脂质体(GSN)配制为递送载体。在阐明和优化配方工艺的基础上,准备了GSL和GSN。结构,累积透射率,皮肤保留,总透光率,并对GSL和GSNs的生物活性进行了表征。GSL和GSN被证明可以抑制人角质形成细胞(HaCaTs)中的脂质过氧化并增加超氧化物歧化酶(SOD)和谷胱甘肽过氧化物酶(GSH-Px)的含量。此外,HaCAT细胞迁移,扩散,和GS细胞摄取显著增加。还在光老化的大鼠模型中评估了GSL和GSN的治疗效果。在用GSL处理的大鼠皮肤中评估组织病理学变化,GSN,或GS通过苏木精-伊红(H&E)和醛品红染色。丙二醛(MDA),SOD,GSH-Px,基质金属蛋白酶(MMPs),白细胞介素-6(IL-6),白细胞介素-1β(IL-1β),并测定肿瘤坏死因子-α(TNF-α)的表达水平。结果表明,GSL的最佳配方是以大豆卵磷脂(SPC)为磷脂,脂质与药物的比例为1:0.4,磷脂与胆固醇的比例为1:3.5。乙醇注射制备GSN的最佳温度为65℃,有机相与水相的比例为1:9。这表明,累积释放率,皮肤保留率,GSL-7在24h的总传输速率高于GSN-4和GS。GSL-7显著抑制由紫外线(UV)辐射引起的皮肤脂质过氧化。此外,GSL-7降低了皮肤组织中MMPs和炎性细胞因子的含量。总之,GSL-7可以减少由UV辐射引起的皮肤老化并有助于皮肤组织修复。
Ginsenosides are the principal bioactive compounds of ginseng. Total ginsenosides (GS) contain a variety of saponin monomers, which have potent anti-photoaging activity and improve the skin barrier function. To enhance the efficiency of GS transdermal absorption, GS liposomes (GSLs) and GS
niosomes (GSNs) were formulated as delivery vehicles. Based on the clarified and optimized formulation process, GSL and GSN were prepared. The structure, cumulative transmittance, skin retention, total transmittance, and bioactivity of GSLs and GSNs were characterized. GSL and GSN were shown to inhibit lipid peroxidation and increase the contents of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) in human keratinocytes (HaCaTs). In addition, HaCAT cell migration, proliferation, and GS cellular uptake were significantly increased. The therapeutic effects of GSL and GSN were also evaluated in a rat model of photoaging. Histopathological changes were assessed in rat skin treated with GSL, GSN, or GS by hematoxylin-eosin (H&E) and aldehyde fuchsine staining. Malondialdehyde (MDA), SOD, GSH-Px, matrix metalloproteinases (MMPs), interleukin-6 (IL-6), interleukin-1β (IL-1β), and tumor necrosis factor-α (TNF-α) expression levels were determined. Results indicated that the optimal formulation of GSL used soybean lecithin (SPC) as the phospholipid, with a lipid-drug ratio of 1:0.4 and a phospholipid-cholesterol ratio of 1:3.5. The optimal temperature for the preparation process of GSN by ethanol injection was 65°C, with a ratio of the organic phase to aqueous phase of 1:9. It was demonstrated that the cumulative release rate, skin retention rate, and total transmission rate of GSL-7 at 24 h were higher than those of GSN-4 and GS. GSL-7 significantly inhibited skin lipid peroxidation caused by ultraviolet (UV) radiation. In addition, GSL-7 reduced the contents of MMPs and inflammatory cytokines in skin tissue. In conclusion, GSL-7 may reduce skin aging caused by UV radiation and contribute to skin tissue repair.