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    黄芩素-锌配合物纳米给药系统的制备及其用于小鼠炎症性肠病的作用研究

    Preparation of the Baicalein-Zinc Complex Nano-delivery System and Effect on Inflammatory Bowel Disease in Mice

      摘要
    • 摘要:
      目的 制备黄芩素-锌(Baicalein-Zinc，Ba-Zn)配合物纳米给药系统，用于治疗小鼠的炎症性肠病(inflammatory bowel disease，IBD)。
      方法 制备Ba-Zn金属配合物，用硫酸软骨素(chondroitin sulfate，CS)修饰后自组装形成Ba-Zn@CS纳米给药系统，采用傅里叶变换红外光谱(Fourier transform infrared spectrometer，FT-IR)、透射电子显微镜(transmission electron microscope，TEM)进行表征，测定其粒径、电位；建立小鼠IBD模型，通过小鼠疾病活动指数(disease activity index，DAI)、结肠长度变化、结肠组织病理学分析等方法评价Ba-Zn@CS纳米给药系统在IBD小鼠体内的药效。
      结果 FT-IR及TEM证明了Ba-Zn@CS的成功合成，其粒径为356.4 nm，多分散性指数(polydispersity index，PDI)为0.129，表面zeta电位为−35.7 mV。体内药效评价显示，Ba-Zn@CS组的小鼠体质量下降情况明显缓解，DAI评分降低，结肠长度大于模型组小鼠(P<0.05)，结肠组织病理检查显示Ba-Zn@CS组的小鼠结肠局部炎症明显缓解。
      结论 Ba-Zn@CS纳米给药系统改善了Ba游离药物的体内抗IBD作用，缓解了IBD小鼠的局部炎症，为提高Ba的生物利用度以治疗IBD提供了新思路。

       

      Abstract:
      OBJECTIVE To prepare Baicalein-Zinc(Ba-Zn) complex nano-delivery system for the treatment of inflammatory bowel disease(IBD) in mice.
      METHODS  The Ba-Zn complex was prepared, and it was modified with chondroitin sulfate(CS) to self-assembly prepare Ba-Zn@CS nano-delivery system. Ba-Zn@CS nanoparticles were characterized by Fourier transform infrared spectrometer(FT-IR) and transmission electron microscope(TEM), and its particle size, potential were determined. The therapeutic effect of the Ba-Zn@CS nano-delivery system was evaluated in the IBD mice from aspects such as the disease activity index(DAI), the length of the colon length, and the pathological analysis of colon tissue pathology.
      RESULTS  FT-IR and TEM proved that the successful construction of Ba-Zn@CS nanoparticles with a particle size of 356.4 nm, polydispersity index(PDI) of 0.129, surface zeta potential of −35.7 mV. The in vivo efficacy evaluation showed that the weight loss of the Ba-Zn@CS treatment group was significantly alleviated, the DAI was reduced, and the colon length was longer than the mice of the model group(P<0.05). The pathological examination of colon tissue showed that the mice in the Ba-Zn@CS treatment group had a significant alleviating local inflammation of the colon.
      CONCLUSION  The Ba-Zn@CS nano-drug delivery system improve the in vivo anti-IBD effect of free Ba drugs, alleviate local inflammation in IBD mice, and provide a new approach to enhance the bioavailability of Ba for the treatment of IBD.

       

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