藤茶总黄酮固体脂质纳米粒抗肝癌活性及其药动学研究  

Anti-hepatoma activity and pharmacokinetics of Ampelopsis grossedentala total flavonoids-loaded solid lipid nanoparticles

作　　者：杨毛毛 罗花彩[2] 徐伟[1] 林珠灿[1] 郭素华[1] 沙玫[1] YANG Mao-mao;LUO Hua-cai;XU Wei;LIN Zhu-can;GUO Su-hua;SHA Mei(College of Pharmacy,Fujian University of Traditional Chinese Medicine,Fuzhou 350122,China;The People’s Hospital Affiliated to Fujian University of Traditional Chinese Medicine,Fuzhou 350004,China)

机构地区：[1]福建中医药大学药学院,福建福州350122 [2]福建中医药大学附属人民医院,福建福州350004

出　　处：《中成药》2020年第9期2249-2254,共6页Chinese Traditional Patent Medicine

基　　金：福建省科技厅引导性项目(2017Y0048,2017Y0050)。

摘　　要：目的评价藤茶总黄酮固体脂质纳米粒抗肝癌活性,并考察其药动学。方法MTT法检测固体脂质纳米粒对HepG2细胞,以及H22荷瘤小鼠肿瘤、体质量、免疫器官的影响。大鼠灌胃给药(150 mg/kg)后于0.167、0.33、0.5、0.667、1、2、3、4、6、8、12、24 h采血,LC-MS/MS法测定二氢杨梅素血药浓度,计算主要药动学参数。结果在24、48、72 h,固体脂质纳米粒对HepG2细胞的IC50值分别为68.63、39.99、32.91μg/mL,低于原料药,并呈浓度依赖性。在0.6、2.4 g/kg剂量下,固体脂质纳米粒对H22荷瘤小鼠的抑瘤率分别为72.22%、59.93%,高于原料药,其Cmax、Tmax、t1/2、AUC0~24 h、AUC0~∞分别是后者的1.76、1.94、2.03、2.80、2.49倍。结论固体脂质纳米粒可提高藤茶总黄酮抗小鼠肝癌活性,并促进其在大鼠体内的口服吸收和生物利用度。AIM To evaluate the anti-hepatoma activity of Ampelopsis grossedentala total flavonoids-loaded solid lipid nanoparticles and to investigate their pharmacokinetics.METHODS MTT assay was applied to detecting the effects of solid lipid nanoparticles on HepG2 cells,and tumor,body weight and immune organs in H22 tumor-bearing mice.Rats were given intragastric administration(150 mg/kg),after which blood collection was performed at 0.167,0.33,0.5,0.667,1,2,3,4,6,8,12,24 h,LC-MS/MS was adopted in the plasma concentration determination of dihydromyricetin,and main pharmacokinetic parameters were calculated.RESULTS At 24,48,72 h,the IC50 values of solid lipid nanoparticles on HepG2 cells were 68.63,39.99,32.91μg/mL,respectively,which were lower than those of raw medicine in a concentration-dependent manner.At the doses of 0.6,2.4 g/kg,the tumor inhibitory rates of solid lipid nanoparticles on H22 tumor-bearing mice were 72.22%,59.93%,respectively,which were higher than those of raw medicine,and the Cmax,Tmax,t1/2,AUC0~24 h,AUC0-∞were 1.76,1.94,2.03,2.80,2.49 times as high as the latter,respectively.CONCLUSION Solid lipid nanoparticles can enhance the anti-hepatoma activity of Ampelopsis grossedentala total flavonoids in mice,and promote their oral absorption and bioavailability in rats in vivo.

关 键 词：藤茶总黄酮 固体脂质纳米粒 抗肝癌活性 药动学 LC-MS/MS 

分 类 号：R285.5[医药卫生—中药学] R969.1[医药卫生—中医学]