马钱子碱固体脂质纳米粒的细胞毒性及细胞摄取试验

Cytotoxicity and Cellular Uptake Test of Brucine-loaded Solid Lipid Nanoparticles

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 investigate cytotoxicity and cellular uptake of brucine-loaded solid lipid nanoparticles （B-SLN） on HepG2 cells. Method： 3- （4, 5-Dimethyhhiazole-2-yl） -2, 5-diphenyhetrazolium- bromide （MTT） assay was used to detect the cytotoxicity of B-SLN on HepG2 cells, the cellular uptake experiments were observed by fluorescence microscopy, flow cytometry was used to detect the cellular uptake of cells under different conditions. Result： Both brucine solution group and B-SLN group had an inhibitory effect on the proliferation of HepG2 ceils, and the inhibition rate increased with increasing of the time and the concentration of brucine, half-inhibitory concentration （IC50） of brucine group in 48, 72 h were 208.5, 78.5 mg·L-^1, iCs0 of B-SLN group in 48, 72 h were 563.3, 114.9 mg·L-^1. When the concentration of brucine was in the range of 125-500 mg·L-^1, with increasing of the drug concentration, the cellular uptake increased from 50.2% to 71.2% ; when the temperature was under the condition of 4 ℃ and 37 ℃ , the cellular uptake increased from 43.0% to 55.2% ; within uptake time of 30-240 min, with the incubation time increasing, the cellular uptake amount increased from 9.7% to 56.4%. Conclusion： SLN administration system can significantly improve the activity of brucine against cancer ceils, B-SLN has the ability to increase cellular uptake of drugs.