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姜黄素载固体脂质纳米粒的抗神经炎症活性及神经毒性评价对 LPS 刺激的 BV-2 小胶质细胞模型。

Antineuroinflammatory Activities and Neurotoxicological Assessment of Curcumin Loaded Solid Lipid Nanoparticles on LPS-Stimulated BV-2 Microglia Cell Models.

机构信息

Department of Integrated Bioscience-Biomedical Chemistry, College of Biomedical and Health Science, Konkuk University, Chungju 27478, Korea.

Nanotechnology Research Center and Department of Integrated Bioscience-Biotechnology, Konkuk University, Chungju 27478, Korea.

出版信息

Molecules. 2019 Mar 25;24(6):1170. doi: 10.3390/molecules24061170.

Abstract

Curcumin, which is a potential antineuroinflammatory and neuroprotective compound, exhibits poor bioavailability in brain cells due to its difficulty in crossing the blood⁻brain barrier and its rapid metabolism during circulation, which decreases its efficacy in treating chronic neuroinflammatory diseases in the central nervous system. The bioavailability and potential of curcumin can be improved by using a nanodelivery system, which includes solid lipid nanoparticles. Curcumin-loaded solid lipid nanoparticles (SLCN) were efficiently developed to have a particle size of about 86 nm and do not exhibit any toxicity in the endothelial brain cells. Furthermore, the curcumin-loaded solid lipid nanoparticles (SLCN) were studied to assess their efficacy in BV-2 microglial cells against LPS-induced neuroinflammation. The SLCN showed a higher inhibition of nitric oxide (NO) production compared to conventional curcumin in a dose-dependent manner. Similarly, the mRNA and proinflammatory cytokine levels were also reduced in a dose-dependent manner when compared to those with free curcumin. Thus, SLCN could be a potential delivery system for curcumin to treat microglia-mediated neuroinflammation.

摘要

姜黄素是一种具有潜在的抗神经炎症和神经保护作用的化合物,但由于其难以穿过血脑屏障和在循环过程中迅速代谢,导致其在大脑细胞中的生物利用度较差,从而降低了其在治疗中枢神经系统慢性神经炎症疾病中的疗效。使用纳米递药系统,包括固体脂质纳米粒,可以提高姜黄素的生物利用度和潜力。本研究成功制备了载姜黄素的固体脂质纳米粒(SLCN),粒径约为 86nm,在脑内皮细胞中没有表现出任何毒性。此外,还研究了载姜黄素的固体脂质纳米粒(SLCN)在 BV-2 小胶质细胞中对抗 LPS 诱导的神经炎症的疗效。结果表明,与常规姜黄素相比,SLCN 以剂量依赖的方式更能抑制一氧化氮(NO)的产生。同样,与游离姜黄素相比,SLCN 也能以剂量依赖的方式降低 mRNA 和促炎细胞因子的水平。因此,SLCN 可能是一种有潜力的姜黄素传递系统,可用于治疗小胶质细胞介导的神经炎症。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1976/6470586/2a138c000fc7/molecules-24-01170-g001.jpg

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