环境响应性"开-关"智能纳米容器的构建及对槐定碱靶向触发释放研究

项目名称： 环境响应性"开-关"智能纳米容器的构建及对槐定碱靶向触发释放研究

项目编号： No.21201098

项目类型： 青年科学基金项目

立项/批准年度： 2013

项目学科： 无机化学

项目作者： 彭海龙

作者单位： 南昌大学

项目金额： 25万元

中文摘要： 槐定碱对肺癌、绒癌和消化道癌等具有较强的治疗作用。前期研究表明，槐定碱采用传统方式给药，在体内分布广，半衰期短，代谢快，生物利用度低，达不到良好的治疗效果，且具有一定的神经毒副作用。本项目利用部分还原沉淀法，核-壳和可逆加成断裂链转移（RAFT）合成技术构建环境响应性"开-关"靶向触发释放智能纳米容器，借助现代分析技术对其性能进行研究。以槐定碱为装载对象，采用体外释放方法探讨温度与交变磁场对释放度的影响。利用磁共振成像扫描技术和药物动力学手段研究纳米容器在动物体内输送行为和靶向机理。根据外加磁场与纳米容器的磁热效应，研究肿瘤组织温度变化与纳米容器释放槐定碱的关系，建立数学模型，实现纳米容器对槐定碱的触发释放。本项目将超顺磁性、环境敏感性及无机纳米材料等概念引入到新型的药物传输载体中，以促进新型药物传输载体的研究和开发。本项目设计思路新颖，与国内外相关工作相比，具有很好的原创性。

中文关键词： 纳米容器；环境响应性；槐定碱；缓控释；靶向

英文摘要： Sophoridine has stronger activities for varous tumor, such as lung cancer, choriocarcinoa and digestive tract cancer. Because of its disadvantages of wide distribution, rapid elimination, low biological half-life and bioavailability in vivo, the clinic efficiency and application of sophoridine were limited. In this study, environmental-responsive and "opening-closing" nanocontainer was fabricated using reductive deposition method, core-shell and RAFT synthesis technology. Meanwhile, the characterization of nanocontainer was investigated by modern analysis techniques. Sophoridine, as the model drug, was loaded by the nanocontainer, and the release properties in vitro was studied by changing temperature and magnetic field. The delivery and targeted mechanism of nanocontainer in vivo was investigated by MRI and pharmacokinetics methods. For realizing trigger-released of sophoridine from the nanocontainer,the relationship between temperature changes of tumor tissue and sophoridine release was studied according to the magnetocaloric effect, and mathematical model was established. In this study, hyperthermia and chemotherapy was used to treat tumor at the same time. The new concepts of superparaagnetic, environmental-responsive and inorganic nanoparticle were introduced into the drug delivery system,which would be im

英文关键词： Nano-container；Environment-responsive；Sophoridine；controlled-releasing；targeted