Synergistic Targeted Delivery of Payload into Tumor Cells by Dual-ligand Liposomes Co-modified with Cholesterol Anchored Transferrin and TAT
Objective: This study was mainly focused on developing a dual-ligand liposomal delivery system to enhance both targeting specificity and cellular uptake.Methods: The specific ligand transferrin (TF) and the cationic cell-penetrating peptide TAT were connected with cholesterol via a polyethylene glycol (PEG) spacer to prepare the dual-ligand liposomes (TAT/TF-PEG-LP).Then the in vitro cellular uptake by three kinds of cells that possessed different expressing levels of transferrin receptor (TFR) was studied.The Ex vivo fluorescence imaging of tumors,the qualitative observation of tumor frozen section and the quantitative determination of cellular uptake in tumor tissues were used to evaluate the in vivo delivery efficiency of TAT/TF-PEG-LP.Results: The result of in vitro cellular uptake showed that TAT/TF-PEG-LP exhibited the enhanced cellular uptake and selectivity via the synergistic effect of both ligands in vitro compared to the single-ligand TAT or TF modified liposomes (TAT-PEG-LP or TF-PEG-LP),The ex vivo fluorescence imaging of tumors,the qualitative and quantitative evaluations of cellular uptake in tumor tissues altogether showed the in vivo delivery efficiency of TAT/TF-PEG-LP was higher than that of other liposomes.Conclusion: the dual-ligand liposomes co-modified with TF and TAT possessed a strong capability for synergistic targeted delivery of payload into tumor cells both in vitro and in vivo.
dual-ligand synergistic effect transferrin cell penetrating peptide
Jie Tang Li Zhang Yayuan Liu Qianyu Zhang Huile Gao Zhirong Zhang Qin He
Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, P. R. China
国内会议
乌鲁木齐
英文
57-61
2013-09-21（万方平台首次上网日期，不代表论文的发表时间）