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

关键词:  黄芩素  配合物  锌  硫酸软骨素  炎症性肠病

Key words:  baicalein  complex  zinc  chondroitin sulfate  inflammatory bowel disease

摘要:

目的 制备黄芩素-锌（Ba-Zn）配合物纳米给药系统，用于治疗小鼠的炎症性肠病（IBD）。方法 制备黄芩素-锌金属配合物，用硫酸软骨素（CS）修饰后自组装形成Ba-Zn@CS纳米给药系统，采用FT-IR、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（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，PDI为0.129，表面zeta电位为-35.7 mV。体内药效评价显示，Ba-Zn@CS组的小鼠体重下降情况明显缓解，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给药系统改善了Ba游离药物的体内抗炎症性肠病作用，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 synthesized, and it was modified with chondroitin sulfate（CS）to prepare Ba-Zn@CS nanoparticles self-assembly. Ba-Zn@CS nanoparticles were characterized by FT-IR and TEM, and its particle size, potential were determined. The therapeutic effect of the Ba-Zn@CS 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, 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 have a significant alleviating local inflammation of the colon. CONCLUSION Ba-Zn@CS NPs exerted significant anti-IBD effects. It provided a new idea for improving Ba's biological utilization to the treatment of IBD.