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植物研究 ›› 2013, Vol. 33 ›› Issue (3): 339-345.doi: 10.7525/j.issn.1673-5102.2013.03.014

• 论文 • 上一篇    下一篇

纳米紫杉醇在人源肠Caco-2细胞模型的吸收转运研究

徐超1,2,3;姜守刚1,2,3;龚显峰4;祖元刚1,2,3*   

  1. 1.生物资源生态利用国家地方联合工程实验室,哈尔滨 150040;2.东北林业大学森林植物生态学教育部重点实验室,哈尔滨 150040;3.东北林业大学林业生物制剂教育部工程研究中心,哈尔滨 150040;4.黑龙江大学化学化工与材料学院,哈尔滨 150040
  • 收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2013-05-20 发布日期:2013-05-20
  • 通讯作者: 祖元刚
  • 基金资助:
     

Nano-paclitaxel Transport by Human Intestinal Epithelial Caco-2 Cells

XU Chao;;JIANG Shou-Gang;;GONG Xian-Feng;ZU Yuan-Gang;*   

  1. 1.State Engineering Laboratory of BioResources EcoUtilization,Northeast Forestry University,Harbin 150040;2.Key Laboratory of Forest Plant Ecology,Ministry of Education,Northeast Forestry University,Harbin 150040;3.Engineering Research Center of Forest Biopreparation,Ministry of Education,Northeast Forestry University,Harbin 150040;4.Institute of Chemistry and Materials Science,Heilongjiang University,Harbin 150040
  • Received:1900-01-01 Revised:1900-01-01 Online:2013-05-20 Published:2013-05-20
  • Contact: ZU Yuan-Gang
  • Supported by:
     

摘要: 大量的研究已经证明,紫杉醇口服吸收较差,容易引起过敏性反应。为了克服紫杉醇的不足,我们制备了一种新的纳米紫杉醇药物,它由甘露醇与人血清白蛋白包裹紫杉醇颗粒制成,其具有更好的水溶性和较低的毒性。为了进一步研究纳米紫杉醇口服给药后的吸收效果,我们利用Caco-2细胞模型对纳米紫杉醇的跨膜转运量进行了测定,3 h内,纳米紫杉醇在0.5~20 μmol·L-1的浓度内的转运量呈线性状态。从膜的顶端到底端的表观渗透系数Papp为(20.9±2.1×10-6 cm·s-1;N=3),米氏方程常数KM值为相对较高的14.00 μmol·L-1,这些数据表明纳米紫杉醇具有更好的吸收效果。

关键词: 纳米紫杉醇, Caco-2细胞模型, 体外转运吸收, P-gp糖蛋白

Abstract: Many studies had proved that oral administration of paclitaxel was poorly absorbed and easy to cause hypersensitivity reactions. For this reason, we produced a new nano-paclitaxel by paclitaxel granule wrapped with mannitol and Human Serum Albumin (HSA), which had better water solubility and lower systemic toxicity. In order to research the absorption of nano-paclitaxel after oral administration, the transepithelial flux of nano-paclitaxel was studied using the human colonic cell line Caco-2 cells. The flux of nano-paclitaxel (at a concentration range of 0.5-20 μmol·L-1) across the Caco-2 cell layer was linear with time for up to 3 h. The apparent permeability coefficient (Papp) for the apical to basolateral transport of nano-paclitaxel (20.9±2.1×10-6 cm·s-1; N=3) and the apparent maximal concentration (KM) of the active efflux component (14.00 μmol·L-1) were relatively high, suggesting that nano-paclitaxel may have a better absorption rate in the intestinal tract.

Key words: nano-paclitaxel, Caco-2 cell, transport absorption, P-glycoprotein

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