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

作　　者：赵晓曄 卜轶卓 张雨晨 何江川 郑云鹤 游翠玉 王珂 ZHAO Xiaoye;BU Yizhuo;ZHANG Yuchen;HE Jiangchuan;ZHENG Yunhe;YOU Cuiyu;WANG Ke(Department of Pharmacy,The First Affiliated Hospital of Xi’an Jiaotong University,Xi’an 710061,China;School of Pharmacy,Xi’an Jiaotong University,Xi’an 710061,China;Department of Thoracic Surgery,The First Affiliated Hospital of Xi’an Jiaotong University,Xi’an 710061,China)

机构地区：[1]西安交通大学第一附属医院药学部,西安710061 [2]西安交通大学药学院,西安710061 [3]西安交通大学第一附属医院胸外科,西安710061

出　　处：《中国现代应用药学》2024年第19期2617-2622,共6页Chinese Journal of Modern Applied Pharmacy

基　　金：国家自然科学基金项目(82204294、32171336);中国医学科学院中央级公益性科研院所基本科研业务费专项资金(2022-JKCS-03)。

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BaZn@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。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.

关 键 词：黄芩素 配合物 锌 硫酸软骨素 炎症性肠病 

分 类 号：R283.6[医药卫生—中药学]