高等学校化学学报 ›› 2010, Vol. 31 ›› Issue (5): 892.

• 研究论文 • 上一篇    下一篇

三氧化二砷磁性纳米粒的表征及其在小鼠组织中的药代动力学

杨国夫1, 李湘晖2, 赵哲1, 刘贾昆1, 王文波1   

  1. 1. 哈尔滨医科大学附属一院骨科;
    2. 哈尔滨医科大学附属二院药学部, 哈尔滨 150001
  • 收稿日期:2009-08-17 出版日期:2010-05-10 发布日期:2010-05-10
  • 通讯作者: 王文波, 男, 博士, 教授, 博士生导师, 主要从事关节置换和肿瘤治疗方面的研究. E-mail: wangwwbo@yahoo.com.cn
  • 基金资助:

    黑龙江省攻关课题(批准号: GC08C421)资助.

Characterization and Tissue Pharmacokinetics in Mice of Arsenic Trioxide Magnetic Nanoparticles

YANG Guo-Fu1, LI Xiang-Hui2, ZHAO Zhe1, LIU Jia-Kun1, WANG Wen-Bo1*   

  1. 1. Department of Orthopaedics, First Affiliated Hospital of Harbin Medical University,
    2. Department of Pharmacy, Second Affiliated Hospital of Harbin Medical University, Harbin 150001, China
  • Received:2009-08-17 Online:2010-05-10 Published:2010-05-10
  • Contact: WANG Wen-Bo. E-mail: wangwwbo@yahoo.com.cn
  • Supported by:

    黑龙江省攻关课题(批准号: GC08C421)资助.

摘要:

通过溶剂转移法制备了三氧化二砷铁氧体磁性纳米粒(As2O3-MNPs). 利用扫描电镜/能谱分析、红外光谱(IR)和差示扫描量热法(DSC)等技术对其进行了表征. 选择正常小鼠肝脏作为靶区, 在外加磁场的诱导下, 考察As2O3-MNPs在小鼠体内的组织药代动力学特征, 以此反映该磁性纳米粒的磁靶向性效果. 红外光谱分析结果显示, As2O3-MNPs中存在磁性材料MgFe2O4; DSC分析表明, 制备磁性纳米粒所用材料As2O3、乳酸羟基乙酸共聚物(PLGA)和铁氧体之间没有明显的相互作用, 可用于磁性纳米粒的制备; 能谱分析结果显示As2O3和磁性材料MgFe2O4 不是吸附于纳米粒的表面, 而是包裹于其中; 磁场组小鼠肝脏组织中药物浓度-时间曲线下面积(AUC0-∞)、达峰浓度(cmax)和消除半衰期(t1/2)均明显大于非磁场组(P<0.05), 说明As2O3-MNPs在正常小鼠体内有良好的磁靶向性分布. 所制备的三氧化二砷磁性纳米粒稳定性好, 靶向性强, 在肿瘤治疗方面具有良好的应用前景.

关键词: 三氧化二砷; 磁性纳米粒; 组织药代动力学

Abstract:

In this study, As2O3-MgFe2O4 magnetic nanoparticles(As2O3-MNPs) were prepared by solvent-displacement method, and their characterization were studied by energy spectrum analysis, IR spectrum analysis and differential scanning calorimetry method(DSC). To guide the external magnetic field in the liver, the tissue pharmacokinetics of As2O3 in mice were also studied. The IR spectrum analysis indicats that there was MgFe2O4 in the As2O3-MNPs. The DSC results show that there was no interaction among As2O3, polylactic-glycolic acid(PLGA) and ferrite. The energy spectrum analysis indicates that MgFe2O4 and As2O3 were not adsorbed on the surface of MNPs but encapsulated in them. The As2O3 MNPs showed good magnetic targeting properties at pharmacokinetics in vivo. The liver tissue concentration-time area under the curve(AUC), peak concentration(cmax), the elimination half-time(t1/2) of the As2O3-MNPs in magnetic group were significantly greater than those in the other group respectively(all P<0.05). So the magnetic targeting effect of As2O3-MNPs was good. As a result, the As2O3-MNPs are promising in chemotherapy of tumor owing to their good stability and magnetic response propertie.

Key words: As2O3 ; Magnetic nanoparticles; Tissue pharmacokinetics

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