School of Function Food and Wine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
Drug Deliv Transl Res. 2024 Mar;14(3):637-654. doi: 10.1007/s13346-023-01418-4. Epub 2023 Sep 11.
This study investigated a nanostructured lipid carrier (NLC)-gel system containing luteolin (LUT), a potential drug delivery system for the treatment of psoriasis. LUT-NLC was prepared by solvent emulsification ultrasonication method. The particle size was 199.9 ± 2.6 nm, with the encapsulation efficiency of 99.81% and drug loading of 4.06%. X-ray diffractometry (XRD), Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) were used to characterize the LUT-NLC. The NLC was dispersed in Carbomer 940 to form the NLC based gel. The rheological characteristics of LUT-NLC-gel showed an excellent shear-thinning behavior (non-Newtonian properties) and coincided with the Herschel-Bulkley model. LUT-NLC-gel (78.89 μg/cm) exhibited better permeation properties and released over 36 hours than LUT gel (32.17 μg/cm). The dye-labeled LUT-NLC presented intense fluorescence in the epidermis and dermis by the visualization of fluorescence and confocal microscopy, and it could accumulate in the hair follicles. The effect of LUT-NLC-gel on imiquimod-induced psoriasis mice was evaluated by psoriasis area severity index scoring, spleen index assay, histopathology, and inflammatory cytokines. These results confirmed that LUT-NLC-gel with high dose (80 mg/kg/day) remarkably reduced the level of inflammatory and proliferation factors such as TNF-α, IL-6, IL-17, and IL-23 in both skin lesions and blood. LUT-NLC-gel improved the macroscopic features. Therefore, the LUT-NLC-gel had great potential as an effective delivery system for skin diseases.
本研究考察了一种含有叶黄素（LUT）的纳米结构化脂质载体（NLC）-凝胶系统，这是一种用于治疗银屑病的潜在药物传递系统。LUT-NLC 通过溶剂乳化超声法制备。粒径为 199.9 ± 2.6nm，包封效率为 99.81%，载药量为 4.06%。X 射线衍射（XRD）、傅里叶变换红外光谱（FTIR）和差示扫描量热法（DSC）用于表征 LUT-NLC。将 NLC 分散在 Carbomer 940 中以形成基于 NLC 的凝胶。LUT-NLC-凝胶的流变特性表现出出色的剪切稀化行为（非牛顿性质），与 Herschel-Bulkley 模型吻合。LUT-NLC-凝胶（78.89μg/cm）表现出更好的渗透性能，释放超过 36 小时，而 LUT 凝胶（32.17μg/cm）释放 32 小时。通过荧光和共聚焦显微镜的可视化，标记有 LUT-NLC 的染料在表皮和真皮中呈现出强烈的荧光，并且可以在毛囊中积累。通过银屑病面积严重程度指数评分、脾指数测定、组织病理学和炎症细胞因子评估 LUT-NLC-凝胶对咪喹莫特诱导的银屑病小鼠的作用。这些结果证实，LUT-NLC-凝胶（高剂量 80mg/kg/天）可显著降低皮肤病变和血液中 TNF-α、IL-6、IL-17 和 IL-23 等炎症和增殖因子的水平。LUT-NLC-凝胶改善了宏观特征。因此，LUT-NLC-凝胶作为一种有效的皮肤病传递系统具有很大的潜力。
