一种新型负载淫羊藿苷的普鲁兰纳米粒制备及其性能研究  

Preparation and performance study of a novel icariin-loaded pullulan nanoparticle

作　　者：何艳娟 陈李凤 雷玉诚 贺宇康 曹志 邹登[1] 邓发文[1] 钟梓妮 袁立明[2] 李湘 HE Yanjuan;CHEN Lifeng;LEI Yucheng;HE Yukang;CAO Zhi;ZOU Deng;DENG Fawen;ZHONG Zini;YUAN Liming;LI Xiang(Department of Pediatrics,The Fourth Hospital of Changsha,Changsha,Hunan 410006,China;School of Medicine,Hunan Normal University,Changsha,Hunan 410000,China)

机构地区：[1]长沙市第四医院儿科,湖南长沙410006 [2]湖南师范大学医学院,湖南长沙410000

出　　处：《湖南中医药大学学报》2024年第8期1385-1390,共6页Journal of Hunan University of Chinese Medicine

基　　金：长沙市自然科学基金项目(kq2202021);湖南省大学生创新创业训练计划项目(S202212652014);湖南师范大学树达学院教学改革项目(院行发教务字[2022]35号6)。

摘　　要：目的 设计一种新型淫羊藿苷修饰的普鲁兰聚合物,通过化学连接和物理包埋的方式高效装载淫羊藿苷,制备一种具有缓释性的纳米球形载体,并对其性能进行初步探讨。方法 淫羊藿苷通过丁二酸酐作为连接臂接枝亲水性普鲁兰形成淫羊藿苷修饰的普鲁兰聚合物,通过傅里叶红外光谱对终产物鉴定。采用透析法制备负载淫羊藿苷的普鲁兰纳米粒。测量空白纳米粒和载药纳米粒的粒径和Zeta电位,利用透射电镜观察其形貌,并测定其在不同pH条件下的体外药物释放行为。结果 纳米粒具有规则的形态、均匀的尺寸。空白纳米粒电位为+2.23 mV,载药纳米粒电位为+3.98 mV;空白纳米粒平均粒径为122 nm,载药纳米粒粒径为190 nm。纳米粒能明显延长淫羊藿苷的缓释作用时间,在pH 6.8的酸性条件下更有利于淫羊藿苷的释放。结论 通过两亲性聚合物自组装行为,成功制备了尺寸均匀的纳米粒。通过聚合物化学连接方式丁二酸将中药单体淫羊藿苷连接普鲁兰制备为纳米递送系统,淫羊藿苷的普鲁兰纳米递送系统该系统能使疏水性药物成为纳米型的水溶性药物,药物具有缓释性,并在弱酸度环境下可以定向释放。Objective To design and preliminarily explore a novel icariin-modified pullulan polymer for efficient loading of icariin via chemical linkage and physical encapsulation,so as to prepare a nanospherical carrier with sustained release properties and investigate its performance.Methods Icariin was grafted onto hydrophilic pullulan via succinic anhydride as a linker arm to form icariin-modified pullulan polymers,and the end products were identified by Fourier infrared spectroscopy.The dialysis method was used to prepare icariin-loaded pullulan nanoparticles.The particle size and zeta potential of the blank and drug-loaded nanoparticles were measured,and their morphology was observed using transmission electron microscopy,and their in vitro drug release behavior was determined under different pH conditions.Results The nanoparticles had regular morphology,uniform size,and homogeneous dimensions.The potential of blank nanoparticles was+2.23 mV,and that of drug-loaded nanoparticles was+3.98 mV;the average particle size of blank nanoparticles was 122 nm,and that of drug-loaded nanoparticles was 190 nm.The nanoparticles could significantly prolong the sustained release time of epimedium glycosides,and it was more favorable for icariin release in the acidic condition of pH 6.8.Conclusion Nanoparticles with uniform size were successfully prepared by amphiphilic polymer self-assembly behavior.The Chinese medicine monomer icariin connected with pullulan was prepared as a nano-delivery system through the polymer chemical linkage mode of succinic acid,and the pullulan nano-delivery system loaded with icariin could make the hydrophobic drug into a nano type of water-soluble drug,and the drug had a slow-release and could be directed to be released under the environment of weak acidity.

关 键 词：淫羊藿苷 普鲁兰多糖 纳米递送系统 药物释放 化学连接 缺血性心肌病 

分 类 号：R283.6[医药卫生—中药学]