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[125I]Spiro-I脑靶向脂质体在小鼠体内分布

周鹤翔, 陈瑞琴, 孙慧, 张沛然, 贾红梅*, 谢英*   

  1. 1. 北京大学 药学院 药剂学系, 北京 100191
    2. 北京师范大学 化学学院, 放射性药物教育部重点实验室, 北京 100875
  • 收稿日期:2009-09-23 修回日期:2009-11-15 出版日期:2010-01-15 发布日期:2010-01-15
  • 通讯作者: 贾红梅*, 谢英*

Bio-distributions of [125I]Spiro-I liposomes in mice

He-Xiang Zhou, Rui-Qin Chen, Hui Sun, Pei-Ran Zhang, Hong-Mei Jia*, Ying Xie*   

  1. 1. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
    2. Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing 100875, China
  • Received:2009-09-23 Revised:2009-11-15 Online:2010-01-15 Published:2010-01-15
  • Contact: Hong-Mei Jia*, Ying Xie*

摘要: 研究[125I]Spiro-I经长循环脂质体(SSL)和脑靶向脂质体(SSTL)包载后的组织分布, 尤其考察其脑摄入。采用薄膜超声分散法制备[125I]Spiro-I脂质体, RMP-7通过共价键连在DSPE-PEG上进一步形成靶向脂质体。[125I]Spiro-I-SSL及SSTL的包封率分别为97.47%±4.01%, 93.02%±2.98%, 粒径分别为(66.47±0.76) nm, (71.40±0.45) nm。给药后, [125I]Spiro-I迅速从血液中清除, 长循环组延长了药物在血液中的保留时间, RMP-7提高了[125I]Spiro-I的脑摄取量。[125I]Spiro-I-SSTL组的AUC较游离药物组提高了1.52倍。SSTL有望拓展显像剂在中枢神经系统的应用。

关键词: [125I]Spiro-I, RMP-7, 脂质体, 组织分布

Abstract: We investigated the bio-distributions of [125I]Spiro-I formulated in sterically stabilized liposomes (SSL) or targeted liposomes (SSTL) in mice, especially their brain uptake. The [125I]Spiro-I liposomes were prepared by film-ultrasound dispersion method. Cereport (RMP-7) was covalently conjugated with DSPE-PEG, which was attached to the surface of SSL to form SSTL. The encapsulation efficiencies (ee%) of [125I]Spiro-I-SSL and [125I]Spiro-I-SSTL were 97.47%±4.01% and 93.02%±2.98%, respectively. The average particle sizes were (66.47±0.76) nm and (71.40±0.45) nm, respectively. After intravenous administration, [125I]Spiro-I was quickly eliminated from blood. SSL could prolong the retention time of [125I]Spiro-I in blood and SSTL improved its brain uptake. The AUC of [125I]Spiro-I-SSTL in brain was increased by 1.52 times as compared to [125I]Spiro-I, indicating that SSTL could be used for the formulation of [125I]Spiro-I for the imaging of central nervous system (CNS).

Key words: [125I]Spiro-I, RMP-7, Liposome, Bio-distribution

中图分类号: 

Supporting:

Foundation items: National Basic Research Program of China (973 Program, Grant No. 2009CB930300); National Natural Science Foundation of China (Grant No.20501004 and 20871021).
*
Corresponding authors. Tel.: 86-10-82801508; e-mail: bmuxieying@bjmu.edu.cn (Y Xie);
Tel.: 86-10-58808891; e-mail: hmjia@bnu.edu.cn (H M Jia)