基于药载一体的甘草外囊泡样颗粒负载甘草查尔酮A纳米给药系统的构建及体外抗炎评价  

Construction and in vitro anti-inflammatory evaluation of a drug-loaded one-piece licorice exocyst-like particle-loaded licorice chalcone A nano-delivery system

作　　者：宁建涛 邓翔 陈莉 杭凌宇 朱煜文 武玲玲 薛玉叶 袁海龙 NING Jian-tao;DENG Xiang;CHEN Li;HANG Ling-yu;ZHU Yu-wen;WU Ling-ling;XUE Yu-ye;YUAN Hai-long(School of Pharmacy,Anhui Medical University,Hefei 230032,China;Department of Pharmacy,Air Force Medical Center,PLA,Air Force Medical University,Beijing 100142,China)

机构地区：[1]安徽医科大学药学院,安徽合肥230032 [2]空军军医大学空军特色医学中心药学部,北京100142

出　　处：《药学学报》2025年第4期1147-1155,共9页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(82174074);空军军医大学领航行动-新飞计划(LH202416)。

摘　　要：本研究以中药甘草来源的外囊泡样颗粒(licorice-derived vesicle-like particles,LVLPs)为载体,以同一来源中药的标志性活性成分——甘草查尔酮A(licochalcone-A,LCA)为模型药物,构建药载一体的外囊泡样纳米给药系统LVLP@LCA,并对其体外特性和抗炎活性进行表征和评价。使用梯度离心法提取外囊泡样纳米颗粒,超声处理装载抗炎药物LCA,制备LVLP@LCA纳米给药系统。制备得到的LVLP@LCA的粒径为160 nm左右,呈茶托状双层膜结构,具有较高的包封率和载药量。体外结果表明,LVLP@LCA进一步增强LCA抑制炎性细胞增殖并降低炎性细胞中ROS和NO水平的能力。同时ELISA和qRT-PCR结果表明,LVLP@LCA能够显著降低IL-6、IL-1β、TNF-α、CCL5、CCL17等相关炎症因子和趋化因子的分泌和mRNA表达。通过蛋白质免疫印迹实验证明,LVLP@LCA通过JAK/STAT通路降低炎症诱导因子IL-6的表达水平,进而抑制炎症反应激活。本研究为甘草药载一体的综合抗炎作用提供理论依据,为中药甘草抗特应性皮炎应用提供一种新思路。In this study,licorice-derived vesicle-like particles(LVLPs)were used as carriers,and licochalconeA(LCA),a signature active ingredient of the same source,was used as a model drug to construct a drug-loaded LVLP@LCA nanodelivery system,and to characterize and evaluate its in vitro properties and anti-inflammatory activity.Licochalcone-A(LCA),a signature active ingredient of traditional Chinese medicine from the same source,was used as a model drug to construct a drug-loaded exocyst-like nano-delivery system,LVLP@LCA,and its in vitro properties and anti-inflammatory activities were characterized and evaluated.The LVLP@LCA nanodelivery system was prepared by extracting the exocyst-like nanoparticles by gradient centrifugation and loading the anti-inflammatory drug LCA by ultrasonication.The LVLP@LCA nanoparticles were prepared with a particle size of about 160 nm and a tea saucershaped bilayer structure,with a high encapsulation rate and drug loading capacity.The in vitro results showed that LVLP@LCA further enhanced the ability of LCA to inhibit the proliferation of inflammatory cells and reduce the levels of ROS and NO in inflammatory cells.Meanwhile,ELISA and qRT-PCR results showed that LVLP@LCA significantly reduced the secretion and mRNA expression of IL-6,IL-1β,TNF-α,CCL5,CCL17 and other related inflammatory factors and chemokines.It was demonstrated by Western blot that LVLP@LCA reduced the expression of inflammation-inducing factor interleukin 6(IL-6)through the JAK/STAT pathway,and then inhibited the activation of inflammatory response.The present study provides a theoretical basis for the comprehensive anti-inflammatory effect of LVLP@LCA and a new way of thinking for the application of Glycyrrhiza glabra as a traditional Chinese medicine against atopic dermatitis.

关 键 词：药载一体 外囊泡样颗粒 甘草查尔酮A 纳米给药系统 抗炎作用 

分 类 号：R943[医药卫生—药剂学]