To construct an artificial low-density lipoprotein (aLDL) that highly mimics low-density lipoprotein (LDL) in vivo, and deliver vincristine (VCR) - doxorubicin (DOX) simultaneously, the 100 nm and 35 nm DOX-VCR-aLDLs (DV-aLDLs) were constructed, then the physicochemical characteristics were evaluated. Through in vitro inverse gravity diffusion experiment, the tumour cake and sphere model experiment, draw a conclusion that the diffusion of 35 nm DV-aLDLs was stronger than 100 nm DV-aLDLs, and the tumour retention of 35 nm DV-aLDLs was better than the DV-solution. In addition, the three-dimension (3D) in vivo distribution imaging of aLDLs was performed on HepG-2 tumour-bearing nude mice, followed by the biodistribution and therapeutic efficacy on these xenograft models. Taking advantage of better diffusion capacity in tumour tissue, as well as the synergistic effect of VCR and DOX, the 35 nm DV-aLDL had the strongest efficacy and the lowest toxicity. High entrapment efficiency and stability, both active and passive targeting, making aLDL a potential carrier for tumour-targeted therapy at the same time.

为构建高度模拟体内低密度脂蛋白 (LDL)并同时递送长春新碱 (VCR) - 阿霉素 (DOX) 的人工低密度脂蛋白 (aLDL)，100 nm 和 35 nm DOX-VCR-aLDL (DV) -aLDLs) 被构建，然后评估其理化特性。通过体外反重力扩散实验、肿瘤饼和球模型实验得出结论：35 nm DV-aLDLs的扩散性强于100 nm DV-aLDLs，35 nm DV-aLDLs的肿瘤滞留性优于35 nm DV-aLDLs。 DV 解决方案。此外，体内三维（3D）在荷 HepG-2 肿瘤的裸鼠上进行 aLDL 分布成像，然后在这些异种移植模型上进行生物分布和治疗效果。利用在肿瘤组织中更好的扩散能力，以及VCR和DOX的协同作用，35 nm DV-aLDL具有最强的疗效和最低的毒性。高包埋效率和稳定性，主动和被动靶向，同时使aLDL成为肿瘤靶向治疗的潜在载体。