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.
NETL
NSTL
万方数据