基于肿瘤整合素ανβ3的靶向分子成像和药物运载系统的深入研究为临床应用奠定了基础。本研究拟以胆固醇、二棕榈酰磷脂酰胆碱及马来酰亚胺-聚乙二醇-二硬脂酰磷脂酰乙醇胺作为膜材，将近红外量子点（Qdot 800）、乳腺癌化疗一线药物表阿霉素（EPB）包裹其中，用拥有自主知识产权的靶向肽P1c进行修饰；优化靶向肽表面密度及纳米脂质体粒径，制备具有诊断和治疗双重功能的靶向量子点纳米脂质体探针。通过激光共聚焦显微镜、流式细胞术、近红外成像等对MDA-MB-231、MCF-7人乳腺癌细胞及脐静脉内皮细胞进行体外结合、亚细胞定位、竞争抑制及细胞杀伤研究；建立ανβ3阳性及阴性人乳腺癌裸鼠模型，用靶向探针实现肿瘤的在体近红外分子成像，观察对荷瘤裸鼠的治疗效果，比较探针在两种模型中的治疗和成像差异；评价靶向肽表面密度及纳米粒径与靶向性的关系，探索同一探针实现诊断与治疗双重作用的可能性。

Molecular imaging and preferential drug delivery system targeting to integrins such as ανβ3 in tumor plays a very important role in diagnosis and treatment of tumor. In this study, membrance materials such as cholesterol (CHOL), dipalmitoylphosphatidyl choline (DPPC), and maleimido-polyethylene glycol2000-distearyl phosphatidyl ethanolamine (Mal-PEG2000-DSPE) are used to prepare a nano-liposome which contain hydrophilic near-infrared quantum dot (Qdot 800) and chemical treatment drug (Epirubicin, EPB) against breast cancer. The liposome is modified with targeting peptide (P1c) with my own intellectual property. Finally, a targeting nano-liposome probe which can be used in both diagnosis and treatment is obtained by optimization of P1c density on liposome surface and nanoparticle size. The characteristics of the probe on human breast cancer lines (MDA-MB-231, MCF-7) and human umbilical vein endothelial cells (HUVECs) such as in vitro specific binding, sub-cellular localization, competitive inhibition, and damage or destructive effect of the probe are investigated by the methods of flow cytometry, Laser confocal microscopy and near-infrared fluorescence(NIRF) imaging. Human breast cancer models with ανβ3 positive and negative expression are established. Treatment effect and NIRF molecular imaging of targeting probe in tumor-bearing nude mice is observed. The differences of imaging and treatment effect between two models and the relationship between targeting of probe and P1c density on liposome surface as well as nanoparticle size are compared. The feasibility that the same probe can have both function of diagnosis and treatment is explored by in vitro and in vivo study.