基于叶酸分子的金属配位纳米药物及药物载体的研究
详细信息 查看官网全文
- 英文论文题名：A folic acid-based metal nanomedicine as well as a drug carrier
- 论文作者：刘理想 ; 李红玫 ; 李祯 ; 李秉霞 ; 董志鹏 ; 王齐彦 ; 王越
- 英文论文作者：Lixiang Liu ; Hongmei Li ; Zhen Li ; Bingxia Li ; Zhipeng Dong ; Qiyan Wang ; Yue Wang ; China Pharmaceutical University
- 年：2016
- 作者机构：中国药科大学;
- 论文关键词：金属纳米药物 ; 靶向 ; 药物载体 ; pH敏感
- 会议召开时间：2016-07-01
- 会议录名称：中国化学会第30届学术年会摘要集-第三十八分会：纳米生物效应与纳米药物化学
- 语种：中文
- 分类号：TQ460.1
- 学会代码：ZGHY
- 会议名称：中国化学会第30届学术年会-第三十八分会 ; 纳米生物效应与纳米药物化学
- 会议地点：中国辽宁大连
- 主办单位：中国化学会
- 学会名称：中国化学会
- 页数：1
- 文件大小：153k
- 原文格式：D
- 会议级别：全国
摘要
纳米技术应用于治疗和药物输送前景广泛,但纳米粒子同时作为肿瘤药物和药物载体鲜有报道。本研究中,有别于传统叶酸(FA)修饰的各类药物载体,我们直接利用生物分子FA与金属钴离子(Co~(2+))配位形成一类具有叶酸受体(FR)靶向性的金属纳米药物,前期体外细胞流式实验表明此类纳米药物对HeLa细胞(FR高表达)的摄取率(98.3%)显著高于正常细胞L-O2(50.6%),细胞活性实验结果显示其对HeLa细胞的抑制作用(IC_(50)=1.47 ug/ml)与阳性药阿霉素(DOX,IC_(50)=0.81ug/ml)相当,而对正常细胞L-O2(IC_(50)=6.98ug/ml)的毒性明显低于DOX(IC_(50)=0.51ug/ml)。此类纳米药物合成方法简便、重现性好,并具有中空管状结构(记为FA-Co NTs,内径5-9 nm,外径10-20 nm,管长150-500 nm,如Fig.1),可用于负载多种抗肿瘤药物(DOX包封率98.1%,载药量38.01%)。FA-Co NTs由配位键构筑,其结构在正常组织中保持相对稳定,具有一定的pH刺激响应性,在靶向至肿瘤微环境(pH=5.0-6.5)处自身结构崩解,实现药物释放,可作为优良的药物载体。
In our study, we utilize folic acid(FA) to coordinate with Co~(2+) to fabricate a new-type metal nanomedicine, in vitro cell experiments indicate that this nanomedicine can target tumor cells and have excellent antitumor activity with low toxicity to normal cells than DOX. Furthermore,the remarkable hollow tubular structure(denoted as FA-Co NTs) give the excellent capacity to load different types of drugs(Drug loading content of DOX is 98.1%, drug loading efficiency is 38.01%). FA-Co NTs are pH-responsive because when they target tumor sites, the coordination bonds are broken and the tubular structure is destroyed due to acidic tumor microenvironment, thus releasing loaded drugs to achieve the more efficient anti-tumor activity.
In our study, we utilize folic acid(FA) to coordinate with Co~(2+) to fabricate a new-type metal nanomedicine, in vitro cell experiments indicate that this nanomedicine can target tumor cells and have excellent antitumor activity with low toxicity to normal cells than DOX. Furthermore,the remarkable hollow tubular structure(denoted as FA-Co NTs) give the excellent capacity to load different types of drugs(Drug loading content of DOX is 98.1%, drug loading efficiency is 38.01%). FA-Co NTs are pH-responsive because when they target tumor sites, the coordination bonds are broken and the tubular structure is destroyed due to acidic tumor microenvironment, thus releasing loaded drugs to achieve the more efficient anti-tumor activity.
引文
[1]Wang,Y.;Zhang,C.;Li,H.M.;Zhu,G.W.;Bao,S.S.;Wei,S.Q.;Zheng,L.M.;Ren,M.;Xu,Z.J.Mater.Chem.B.2015,3:296.
[2]Gao,P.F.;Zheng,L.L.;Liang,L.J.;Yang,X.X.;Li,Y.F.;Huang,C.Z.J.Mater.Chem.B.2013,1:3202.
[2]Gao,P.F.;Zheng,L.L.;Liang,L.J.;Yang,X.X.;Li,Y.F.;Huang,C.Z.J.Mater.Chem.B.2013,1:3202.