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Biotin and glucose dual-targeting, ligand-modified liposomes promote breast tumor-specific drug delivery.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-03-29 , DOI: 10.1016/j.bmcl.2020.127151 Mengyi Huang 1 , Yanchi Pu 1 , Yao Peng 1 , Qiuyi Fu 1 , Li Guo 1 , Yong Wu 1 , Yongxiang Zheng 2
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-03-29 , DOI: 10.1016/j.bmcl.2020.127151 Mengyi Huang 1 , Yanchi Pu 1 , Yao Peng 1 , Qiuyi Fu 1 , Li Guo 1 , Yong Wu 1 , Yongxiang Zheng 2
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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.
中文翻译：
生物素和葡萄糖双重靶向，配体修饰的脂质体可促进乳腺肿瘤特异性药物的递送。
乳腺癌是女性与癌症相关的死亡的第二大主要原因。配体修饰的脂质体可用于乳腺肿瘤特异性药物递送，以提高疗效并减少化疗的副作用；然而，仅开发了少数具有高靶向效率的脂质体，因为单靶向配体修饰的脂质体通常不能递送足够的治疗剂量。在这项研究中，我们设计了生物素葡萄糖分支配体修饰的双靶向脂质体（Bio-Glu-Lip），并评估了它们作为体外和体内靶向化疗药物递送系统的潜力。与非靶向脂质体（Lip），Bio-Lip和Glu-Lip相比，Bio-Glu-Lip在4T1细胞中具有最高的细胞摄取（分别高3.00倍，1.60倍和1.95倍） ）和MCF-7细胞（2.63倍，1.63倍和1。分别高出85倍）。随后的细胞毒性和体内测定进一步支持了双靶脂质体是用于乳腺癌治疗的有希望的药物递送载体。
更新日期：2020-03-29
中文翻译：
生物素和葡萄糖双重靶向，配体修饰的脂质体可促进乳腺肿瘤特异性药物的递送。
乳腺癌是女性与癌症相关的死亡的第二大主要原因。配体修饰的脂质体可用于乳腺肿瘤特异性药物递送，以提高疗效并减少化疗的副作用；然而，仅开发了少数具有高靶向效率的脂质体，因为单靶向配体修饰的脂质体通常不能递送足够的治疗剂量。在这项研究中，我们设计了生物素葡萄糖分支配体修饰的双靶向脂质体（Bio-Glu-Lip），并评估了它们作为体外和体内靶向化疗药物递送系统的潜力。与非靶向脂质体（Lip），Bio-Lip和Glu-Lip相比，Bio-Glu-Lip在4T1细胞中具有最高的细胞摄取（分别高3.00倍，1.60倍和1.95倍） ）和MCF-7细胞（2.63倍，1.63倍和1。分别高出85倍）。随后的细胞毒性和体内测定进一步支持了双靶脂质体是用于乳腺癌治疗的有希望的药物递送载体。
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