Liu Xing, Shu Wenlin, Zhong Qingrui, Zeng Anqi, Zeng Yong, Gu Huan, Chen Ping, Li Xiaofang
State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, People's Republic of China.
Translational Chinese Medicine Key Laboratory of Sichuan Province, Sichuan Academy of Chinese Medicine Sciences, Chengdu, 610041, People's Republic of China.
Int J Nanomedicine. 2025 Jun 19;20:7935-7951. doi: 10.2147/IJN.S516572. eCollection 2025.
PURPOSE: Prolonged exposure of the skin to ultraviolet (UV) rays from sunlight causes oxidative damage to skin cells, and prolonged exposure to UV can lead to severe sunburn and skin aging, which may increase the risk of skin cancer. Numerous natural products have been used to treat UV-induced skin damage. Baicalin (BA) has excellent antioxidant properties; however, its poor solubility hinders its direct application. Therefore, suitable formulations for dermal administration must be developed. METHODS: We designed a temperature-sensitive gel drug delivery system based on baicalin liposome (BA-LP), which was first constructed using lecithin loaded with insoluble BA. Subsequently, an injectable hydrogel (BA-LG) with temperature-sensitive properties was constructed using BA-LP and chitosan (CS) with β-glycerophosphate tetrahydrate (β-GP) as a crosslinking agent. RESULTS: BA-LP had homogeneous particle size, high EE, and good stability. BA-LG could be gelled within 2 min at 37 °C and had good spreading, adhesion, and injectability properties. The in vitro release results showed that BA-LG had a significantly slower release effect, with a cumulative release of 60% at 24 h. The effects of BA-LG on skin keratinocyte HaCaT cells were evaluated using the CCK8 method and transwell co-culture, and the results showed good cell activity and a high survival rate, indicating that the hydrogel has good biosafety. In the UVB-induced skin injury mouse model, BA-LG showed significant effects by increasing superoxide dismutase (SOD) activity, decreasing malondialdehyde (MDA) damage, and inhibiting the expression of inflammatory factors IL-6, PGE2, and TNF-α, and demonstrated a superior therapeutic effect. The analysis of histopathological sections of the skin stained with H&E and Masson revealed results consistent with those observed on the mice. CONCLUSION: In summary, our results suggest that BA-LG, a temperature-sensitive gel based on baicalin liposomes, has good therapeutic efficacy and potential applications in the treatment of UVB-induced skin damage.
目的：皮肤长时间暴露于阳光中的紫外线（UV）会对皮肤细胞造成氧化损伤，长期暴露于紫外线会导致严重晒伤和皮肤老化，这可能会增加患皮肤癌的风险。许多天然产物已被用于治疗紫外线引起的皮肤损伤。黄芩苷（BA）具有出色的抗氧化性能；然而，其溶解性差阻碍了其直接应用。因此，必须开发适合皮肤给药的制剂。 方法：我们设计了一种基于黄芩苷脂质体（BA-LP）的温度敏感凝胶药物递送系统，首先使用负载不溶性BA的卵磷脂构建该脂质体。随后，以BA-LP和壳聚糖（CS）为原料，以四水合β-甘油磷酸酯（β-GP）作为交联剂，构建了具有温度敏感性的可注射水凝胶（BA-LG）。 结果：BA-LP粒径均匀，包封率高，稳定性好。BA-LG在37℃下2分钟内即可凝胶化，具有良好的铺展性、粘附性和可注射性。体外释放结果表明，BA-LG具有明显较慢的释放效果，24小时累积释放率为60%。采用CCK8法和transwell共培养法评价BA-LG对皮肤角质形成细胞HaCaT细胞的影响，结果显示细胞活性良好，存活率高，表明该水凝胶具有良好的生物安全性。在紫外线B诱导的皮肤损伤小鼠模型中，BA-LG通过提高超氧化物歧化酶（SOD）活性、降低丙二醛（MDA）损伤以及抑制炎症因子IL-6、PGE2和TNF-α的表达显示出显著效果，并表现出优异的治疗效果。对用苏木精和伊红（H&E）及Masson染色的皮肤组织病理切片分析显示结果与在小鼠身上观察到的结果一致。 结论：总之，我们的结果表明，基于黄芩苷脂质体的温度敏感凝胶BA-LG在治疗紫外线B诱导的皮肤损伤方面具有良好的治疗效果和潜在应用价值。
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