摘要
目的研究新型高分子材料Chol-PEG-GA修饰马钱子碱脂质体(CPGL)体外肝癌细胞摄取特性。方法采用硫酸铵梯度法制备马钱子碱普通脂质体(LP)和CPGL,测定其包封率,以人肝癌SMMC-7721细胞株为模型,研究孵化温度、给药剂量、Chol-PEG-GA及甘草次酸浓度等因素对LP和CPGL摄取的影响。结果 LP和CPGL的平均包封率分别为(81.5±1.2)%和(86.8±1.6)%,平均粒径分别为(131.3±15.8)nm和(147.2±16.6)nm。经过60 min孵育,肝癌细胞摄取CPGL的单位蛋白摄取量高于LP;在25～100 mg.L-1药物浓度范围内,肝癌细胞摄取CPGL的单位细胞摄取马钱子碱量随给药剂量的增加而增加,且明显高于LP(P<0.05)。4℃温度条件下,单位蛋白摄取量明显低于37℃,有显著差异(P<0.05)。结论CPGL可作为肝细胞靶向的载体,显著提高药物进入肝癌细胞的摄取量,为临床治疗肝脏疾病提供理论依据。
AIM To investigate the brucine modified liposomes with the new polymer material Chol-PEG- GA （CPGL） as a targeting carrier in hepatic cells by increasing the accumulation of brucine. METHODS brucine liposomes （LP） and CPGL were prepared by ammonium sulfate gradient method, and the entrapment efficiency of LP and CPGL was determined. The uptakes of CPGL and LP were studied in human SMMC-7721 hepatocellular carcinoma cells in vitro, such as the influence of incubation temperature, the dose, the concentration of CPGL, and the addition of glycyrrhetinic acid. RESULTS The entrapment efficiency of LP and CPGLwas （81.5 ± 1.2） % and （86.8 ± 1.6） %; the mean size was （131.3 ± 15.8） nm and （147.2 ± 16.6） nm, respectively. After incubation 60 min, cellular uptake of CPGL was higher than that of LP. Ranging from 25 mg. L^-1 to 100 mg.L^-1, the uptake of CPGL was increased along with the dose, and was higher than that of LP （P 〈 0.05）. The uptake of CPGL at 4℃ was lower than that at 37 ℃ （P 〈 0.05）. CONCLUTION Brucine modified with glycyrrhetinie acid as a targeting carrier can improve the uptake significantly, which theoretical foundation for further clinical therapy. liposome provides
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2012年第1期16-20,共5页
Chinese Journal of New Drugs and Clinical Remedies
基金
教育部新教师基金资助项目(20093237120016)
南京中医药大学青年自然科学基金资助项目(09XZR16)
关键词
甘草次酸
马钱子碱
脂质体
肝癌细胞株
体外研究
glycyrrhetinic acid
brucine
liposomes
hepatocellular carcinoma cell
in vitro
