多功能近红外荧光给药复合纳米胶囊的制备与应用

项目名称： 多功能近红外荧光给药复合纳米胶囊的制备与应用

项目编号： No.21475007

项目类型： 面上项目

立项/批准年度： 2015

项目学科： 数理科学和化学

项目作者： 汪乐余

作者单位： 北京化工大学

项目金额： 89万元

中文摘要： 恶性肿瘤严重威胁人类健康，大剂量化疗药物对正常组织产生极强毒副作用。探索既能实现抗癌药物的靶向缓释、集化疗与热疗于一体、又能实时观察肿瘤药物疗效的多功能复合纳米抗癌胶囊，意义重大。本项目拟以热敏高分子将抗癌药物（用于肿瘤化疗）、近红外光热转换纳米颗粒（用于近红外光热转换热疗）及近红外荧光纳米晶（用于近红外荧光成像）包覆成多功能复合胶囊，并以功能多肽对胶囊表面进行修饰（用于定向纳米胶囊到达肿瘤部位）。在近红外光（808纳米）照射下，光热转换纳米颗粒可吸收近红外光转变成热，使肿瘤因受热而被杀死；同时，温敏高分子层在受热作用下会收缩，进而将抗癌药物挤出胶囊而产生化疗作用；此外，荧光纳米颗粒则在光照下发射红外荧光，利用红外荧光(无背景荧光干扰、组织穿透深、适合活体成像)可对肿瘤进行荧光成像、实时监控肿瘤大小和抗癌治疗效果。以期为癌症等重大疾病的靶向缓释治疗提供新材料、新技术和新方法。

中文关键词： 复合纳米胶囊；近红外荧光；细胞成像；活体成像；药物缓释

英文摘要： Recently, malignant tumour threatens people's health seriously. As we know, the chemical anti-cancer drugs have played an important role on the therapy of cancers. However, high-dose chemotherapy drugs also have strong side effects on normal tissues. The increasing need for drug delivery systems that improve specificity and activity and at the same time reduce toxicity to ensure maximum treatment safety has led to the development of a great variety of drug vectors. The development of a multifunctional nanocomposite capsule which is capable of targeted and controlled chemotherapy drug release, photothermal therapy, and in-situ monitoring the efficacy of the cancer therapy, is highly desirable. Herein, via a facile strategy, chemotherapy drugs, nanoparticles with NIR photothermal therapy ability, and the nanocrystals with near-infrared (NIR) fluorescence will be encapsulated in the thermoresponsive polymer nanosphere to form the multifunctional nanocapsule. With the guidance of functional peptides bioconjugated onto the surface of the nanospheres, these multifunctional nanocapsules can be targeted to the tumour. Under the NIR (808nm) light irradiation, the photothermal nanoparticles (NPs) will convert light energy into heat, which on the one hand will kill the tumor via the increased temperature, and on the other hand will induce the thermosensitive polymer shell to shrink and the encapsulated drugs will be released. The tumor will be killed by means of both photothermal therapy and chemotherapy. Meanwhile, the fluorescent NPs will emit strong NIR fluorescence with the 808 nm irradiation, which can be utilized for the tumor fluorescence imaging to indicate the tumor size and thus used for the in-situ evaluation of the tumor therapy. It is notable that the NIR has many advantages including low autofluorescence background and high penetration depth, which is highly desirable for the in-vivo imaging. In summary, we hope these researches will find potential applications in the multimodality treatment of tumors and other serious diseases.

英文关键词： nanocomposite;near infrared fluorescence;cell imaging;in vivo imaging;drug delivery