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目的:研究马钱子碱固体脂质纳米粒(brucine-loaded solid lipid nanoparticles,B-SLN)对Hep G2的细胞毒性和细胞摄取情况。方法:采用四甲基偶氮唑盐比色法(MTT)检测B-SLN对Hep G2细胞的毒性,利用荧光显微镜定性观察细胞摄取情况,运用流式细胞仪定量检测不同条件下的细胞摄取情况。结果:马钱子碱组和B-SLN组对Hep G2细胞增殖具有抑制作用,且抑制率随时间延长和药物质量浓度增加而上升。马钱子碱组48,72 h的半抑制浓度(IC_(50))分别为208.5,78.5 mg·L~(-1),B-SLN组48,72 h的IC50分别为563.3,114.9 mg·L~(-1);药物质量浓度在125~500 mg·L~(-1)时,随药物质量浓度的增加,细胞摄取量由50.2%增加到71.2%;温度在4℃和37℃条件下,细胞摄取量由43%增加到55.2%;摄取时间在30~240 min时,随孵育时间的增加,细胞摄取量由9.7%增加到56.4%。结论:SLN给药系统能显著提高马钱子碱对抗癌细胞的活性,且B-SLN具有增加药物被细胞摄取的能力。
Objective: To study the cytotoxicity and cellular uptake of Hep G2 by brucine-loaded solid lipid nanoparticles (B-SLN). Methods: The cytotoxicity of B-SLN to Hep G2 cells was detected by MTT assay. The uptake of B-SLN was detected by fluorescence microscopy. The uptake of cells under different conditions was quantified by flow cytometry . Results: The strychnine group and the B-SLN group had an inhibitory effect on the proliferation of Hep G2 cells, and the inhibition rate increased with the prolongation of time and the increase of the drug concentration. The half-inhibitory concentration (IC 50) of strychnine group at 208 and 72 h were 208.5 and 78.5 mg · L -1, respectively. The IC50 of strychnine group at 48 and 72 h were 563.3 and 114.9 mg · L ~ (-1). When the drug concentration was in the range of 125 ~ 500 mg · L -1, the cellular uptake increased from 50.2% to 71.2% with the increase of the drug concentration; at 4 ℃ and 37 ℃ , The cell uptake increased from 43% to 55.2%, and the cell uptake increased from 9.7% to 56.4% with the increase of incubation time from 30 to 240 min. CONCLUSIONS: SLN administration system can significantly increase the activity of brucine against cancer cells, and B-SLN has the ability to increase drug uptake by cells.