Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China; Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Sichuan Engineering Laboratory for Plant-Sourced Drug, Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China.
Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China; Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Sichuan Engineering Laboratory for Plant-Sourced Drug, Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China; Department of Biopharmaceutics, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China.
Bioorg Med Chem Lett. 2020 Jun 15;30(12):127151. doi: 10.1016/j.bmcl.2020.127151. Epub 2020 Mar 29.
Breast cancer is the second leading cause of cancer-related deaths in women. Ligand-modified liposomes are used for breast tumor-specific drug delivery to improve the efficacy and reduce the side effects of chemotherapy; however, only a few liposomes with high targeting efficiency have been developed because the mono-targeting, ligand-modified liposomes are generally unable to deliver an adequate therapeutic dose. In this study, we designed biotin-glucose branched ligand-modified, dual-targeting liposomes (Bio-Glu-Lip) and evaluated their potential as a targeted chemotherapy delivery system in vitro and in vivo. When compared with the non-targeting liposome (Lip), Bio-Lip, and Glu-Lip, Bio-Glu-Lip had the highest cell uptake in 4T1 cells (3.00-fold, 1.60-fold, and 1.95-fold higher, respectively) and in MCF-7 cells (2.63-fold, 1.63-fold, and 1.85-fold higher, respectively). The subsequent cytotoxicity and in vivo assays further supported the dual-targeting liposome is a promising drug delivery carrier for the treatment of breast cancer.
乳腺癌是女性癌症相关死亡的第二大主要原因。配体修饰的脂质体用于乳腺癌肿瘤特异性药物递送，以提高疗效并降低化疗的副作用；然而，由于单靶向配体修饰的脂质体通常无法递送足够的治疗剂量，因此仅开发了少数具有高靶向效率的脂质体。在本研究中，我们设计了生物素-葡萄糖支化配体修饰的双靶向脂质体（Bio-Glu-Lip），并评估了它们作为靶向化疗药物递送系统在体外和体内的潜力。与非靶向脂质体（Lip）、Bio-Lip 和 Glu-Lip 相比，Bio-Glu-Lip 在 4T1 细胞（分别高 3.00 倍、1.60 倍和 1.95 倍）和 MCF-7 细胞（分别高 2.63 倍、1.63 倍和 1.85 倍）中的细胞摄取率最高。随后的细胞毒性和体内实验进一步证实，双靶向脂质体是治疗乳腺癌的一种有前途的药物递送载体。
