Department of Physiology, School of Basic Medical Sciences, Hubei University of Science and Technology, Xianning 437100, China.
Department of Pharmaceutics, School of Pharmacy, Hubei University of Science and Technology, Xianning 437100, China.
Molecules. 2024 Feb 29;29(5):1081. doi: 10.3390/molecules29051081.
Lycorine is a kind of natural active ingredient with a strong antitumor effect. In this study, folate ligand-conjugated polyethylene glycol-block-poly(l-lactide) (PEG-PLLA) nanoparticles (FA-PEG-PLLA NPs) were designed to deliver lycorine to enhance its anti-glioma activity. The successful preparation of the FA-PEG-PLLA polymer was confirmed by H-NMR, FT-IR, XRD, TGA, and DSC. The optimal formulation for LYC@FA-PEG-PLLA NPs was determined by response surface analysis as follows: sodium dodecyl sulfate (SDS) of 1%, carrier material of 0.03 g, organic phase volume of 3 mL, and ultrasonic power of 20%. The LYC@FA-PEG-PLLA NPs exhibited an encapsulation efficiency of 83.58% and a particle size of 49.71 nm, demonstrating good stability. Hemolysis experiments, MTT assays, and cell scratch assays revealed excellent biocompatibility of FA-PEG-PLLA and superior anti-glioma activity of LYC@FA-PEG-PLLA NPs compared to the raw drug. Additionally, cell apoptosis assays, ROS experiments, and western blot analysis demonstrated that LYC@FA-PEG-PLLA NPs contributed to cell apoptosis by inducing ROS generation and increasing the expression of NF-κB inhibitory protein IκBα. These results suggested that LYC@FA-PEG-PLLA NPs hold promise for glioma treatment.
石蒜碱是一种具有较强抗肿瘤作用的天然活性成分。本研究设计了叶酸配体修饰的聚乙二醇-聚（L-乳酸）（PEG-PLLA）纳米粒（FA-PEG-PLLA NPs）来递送石蒜碱，以增强其抗神经胶质瘤活性。通过 1 H-NMR、FT-IR、XRD、TGA 和 DSC 证实了 FA-PEG-PLLA 聚合物的成功制备。通过响应面分析确定了 LYC@FA-PEG-PLLA NPs 的最佳配方如下：十二烷基硫酸钠（SDS）为 1%，载体材料为 0.03 g，有机相体积为 3 mL，超声功率为 20%。LYC@FA-PEG-PLLA NPs 的包封效率为 83.58%，粒径为 49.71 nm，表现出良好的稳定性。溶血实验、MTT 实验和细胞划痕实验表明，FA-PEG-PLLA 具有良好的生物相容性，LYC@FA-PEG-PLLA NPs 的抗神经胶质瘤活性优于原料药。此外，细胞凋亡实验、ROS 实验和 Western blot 分析表明，LYC@FA-PEG-PLLA NPs 通过诱导 ROS 生成和增加 NF-κB 抑制蛋白 IκBα的表达促进细胞凋亡。这些结果表明，LYC@FA-PEG-PLLA NPs 有望用于治疗神经胶质瘤。
