Ligand-Switchable Micellar Nanocarriers for Prolonging Circulation Time and Enhancing Targeting Efficiency

Cheng, TJ (Cheng, Tangjian)^[ 1,2 ] ; Zhang, YM (Zhang, Yumin)^[ 3,4 ] ; Liu, JJ (Liu, Jinjian)^[ 3,4 ] ; Ding, YX (Ding, Yuxun)^[ 1,2 ] ; Ou, HL (Ou, Hanlin)^[ 1,2 ]; Huang, F (Huang, Fan)^[ 3,4 ] ; An, YL (An, Yingli)^[ 1,2 ] ; Liu, Y (Liu, Yang)^[ 1,2 ] ; Liu, JF (Liu, Jianfeng)^[ 3,4 ] ; Shi, LQ (Shi, Linqi)^[ 1,2 ]

ACS APPLIED MATERIALS & INTERFACES, 2018, 10(6): 5296-5304

DOI: 10.1021/acsami.7b18137

 WOS:000425572700017

Abstract

Targeted drug delivery of nanomedicines offered a promising strategy to improve the tumor accumulation and reduce the side effects of chemotherapeutics. However, undesired recognition of the targeting ligands on the surface of nanocarriers, by immune systems or normal tissues decreased the circulation time and reduced the targeting efficiency. Here, we developed a ligand-switchable micellar nanocarrier that can hide the targeting ligands when circulating in the bloodstream and expose them on the surface when entering the tumor microenvironments. With the ligandswitching capability, the nanocarrier achieved a 66% longer blood circulation half-life and a 23% higher tumor accumulation than the nanocarrier with targeting ligands on the surface. This targeting strategy could serve as a universal approach to improve the targeting efficiency for nanomedicines.