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作 者:马哲 吴超 陈健 MA Zhe;WU Chao;CHEN Jian(Jinzhou Medical University,Jinzhou 121001 ,China;The 205 Hospital of the Chinese People's Liberation Army,Jinzhou 121001,China)
机构地区:[1]锦州医科大学,辽宁锦州121001 [2]中国人民解放军第二〇五医院,辽宁锦州121001
出 处:《中国药学杂志》2019年第2期110-116,共7页Chinese Pharmaceutical Journal
摘 要:目的构建透明质酸(hyaluronan hyaluronic acid,HA)功能化MCM-41型介孔二氧化硅纳米粒(MCM-41)包载紫杉醇(paclitaxel,PTX)的靶向药物递送系统(HA-MCM-41-PTX)。考察其理化性质、体外释药行为及体外肿瘤抑制效果。方法通过透射电镜考察MCM-41的形态结构及粒径,粉末X射线衍射法和傅里叶红外光谱法对载药体系进行表征,体外溶出实验考察载药体系的体外释放行为,体外细胞实验探究载药体系对SMMC-7721细胞的作用机制。结果 HA-MCM-41-PTX载药量为26. 75%。体外释药呈缓释,48 h药物累积释放量为(86. 19±5. 11)%。细胞实验表明,载药体系具有靶向作用,易被细胞摄入并表现出良好的肿瘤细胞抑制作用。结论 HA-MCM-41-PTX是同时具有缓释性和靶向性的载药体系。OBJECTIVE To establish a drug delivery system based on hyaluronic acid functionalized mesoporous silica nanoparticles MCM-41 loaded with paclitaxel(HA-MCM-41-PTX).The physical and chemical properties,in vitro drug release and the antitumor effect were investigated.METHODS The morphological structure and particle size of MCM-41 were observed by TEM.The drug delivery system was characterized by PXRD and FTIR.The in vitro release experiments was carried out to investigate the dissolution rate of HA-MCM-41-PTX.The in vitro cells experiment was carried out to explore the mechanism of HA-MCM-41-PTX on cells.RESULTS The drug loading capacity of HA-MCM-41-PTX was 28.75%.The in vitro drug release experiments showed that HA-MCM-41-PTX exhibited controlled release with a cumulative release of(86.19±5.11)%until 48 h.In vitro cell experiments showed that HA-MCM-41-PTX had excellent targeting effect due to the modification of hyaluronic acid,which was easier to be uptaken by cells and exhibited great antitumor effect.CONCLUSION HA-MCM-41-PTX is an excellent drug delivery system with both controlled release and targeting antitumor effect.
关 键 词:透明质酸 介孔二氧化硅 SMMC-7721肝癌细胞 紫杉醇 肿瘤
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