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活体成像系统检测甘草次酸修饰脂质体在小鼠体内的分布
  • ISSN号:1005-9903
  • 期刊名称:《中国实验方剂学杂志》
  • 时间:0
  • 分类:R284.1[医药卫生—中药学;医药卫生—中医学] R285.5[医药卫生—中药学;医药卫生—中医学]
  • 作者机构:[1]南京中医药大学药学院,南京210046, [2]南京中医药大学国家教育部中药炮制规范化及标准化工程研究中心,南京210029, [3]南京海昌中药集团,南京210061, [4]中国药科大学,南京210009
  • 相关基金:教育部新教师基金项目(20093237120016);南京中医药大学青年自然科学基金项目(09XZR16)
中文摘要:

目的:研究胆固醇-聚乙二醇-甘草次酸(Chol—PEG—GA)修饰脂质体(CPGL)在小鼠体内的长循环型和分布情况,为肝肿瘤的靶向治疗提供理论依据。方法:将普通脂质体(LP)和CPGL分别包裹荧光显像剂NIRD-15,通过NIRD-15跟踪检测LP和CPGL在小鼠体内分布情况。将小鼠随机分为LP组和CPGL组,分别尾静脉注射,与药物注射后5,10,15,30,60,120,180,360,600min采用活体成像系统观察小鼠活体及离体器官中药物荧光强度。结果:尾静脉注射LP后随循环系统迅速分布到各器官,肝靶向性较差。尾静脉注射CPGL15min后,药物开始聚集在肝脏,600min后在肝脏中的药物浓度仍显著高于LP组,说明用Chol—PEG—GA修饰的脂质体能主动靶向于肝细胞,并延长其在肝组织的滞留时间。结论:CPGL在体内有明显的长循环性和肝靶向性,延长其在体内的半衰期,减少药物代谢率,靶向到达肝脏,延长在肝脏的滞留时间。

英文摘要:

choesterol-poly ( To prove the long-circulating and distribution of liposome which is modified with 2000-glycyrrhetinic acid (Chol-PEG-GA) (CPGL) in vivo and provide theoretical or. Method: The biodistribution of NIRD-15 labeled liposome was studied in mice The mice were randomly separated in conventional liposomes (LP) group and ntensities in vivo and in isolated organs were measured 5, 10, 15, 30, 60, 120, Objective : ethylene glycol) 180, 360, 600 min after injection. Result: LP faded away quickly through metabolism in organs of body, transferred by circulation system, while few phenomenon of NIRD-15' s enrichment in-liver occurred. After injected CPGL into body, the content ratio of NIRD-15 in the body was increased slowly. The phenomenon of NIRD-15 enrichment occurred in the liver 15 min after administration, and the concentration was still higher than LP after 600 min, which suggested liposomes modified with Chol-PEG-GA can target to the liver and extend its residence time in liver. Conclusion: CPGL can control the release of the drug in vivo, prolong the biological half life, and improve the liver targeting effect.

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期刊信息
  • 《中国实验方剂学杂志》
  • 北大核心期刊(2011版)
  • 主管单位:国家中医药管理局
  • 主办单位:中国中医科学院中药研究所 中华中医药学会
  • 主编:吴以岭
  • 地址:北京东直门内南小街16号中国中医科学院中药研究所304室
  • 邮编:100700
  • 邮箱:syfjx_2010@188.com
  • 电话:010-84076882
  • 国际标准刊号:ISSN:1005-9903
  • 国内统一刊号:ISSN:11-3495/R
  • 邮发代号:2-417
  • 获奖情况:
  • 全国中医药优秀期刊三等奖,首届《CAJ-CD规范》执行优秀奖
  • 国内外数据库收录:
  • 美国化学文摘(网络版),中国北大核心期刊(2008版),中国北大核心期刊(2011版),中国北大核心期刊(2014版)
  • 被引量:59476