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Accurate Targeting and Controllable Release of Hybrid Liposome Containing a Stretchable Copolymer

Year: 2020

Journal: Macromol. Chem. Phys., Volume 221, APR

Authors: Wang, YZ; Lei, B; Sun, MJ; Han, X; Xu, SH; Liu, HL

Organizations: National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21776071, 21878075]; Innovative Research Group Project of the National Natural Science Foundation of China (CN)National Natural Science Foundation of China (NSFC) [51621002]

Keywords: controllable drug release; Langmuir-Blodgett films; multistage responsive liposomes; pH-; temperature dual-sensitive copolymers

Developing an intelligent drug delivery/release system, which can transport drugs to the target tissues precisely and release drugs timely, is an important challenge in chemotherapy. A multistage sensitive drug delivery system is designed by inserting a folate (FA) modified lipid and a pH/temperature dual-sensitive amphiphilic copolymer into a liposome bilayer. The stretchable copolymer plays a role in protection on FA ligand for more accurate targeting. Then, the stretch ability of the copolymer in the liposome bilayer is verified by using the Langmuir-Blodgett film technique. The interaction between the 1,2-dipalmitoyl-sn-glycerol-3-phosphocholine (DPPC) monolayer and hybrid liposomes is found to increase, indicating the FA ligand is exposed due to the copolymer shrinking with increasing temperature. Fluorescence polarization measurements demonstrate that the insertion of the copolymer improves the stability of the liposome and offers pH-controllability for drug release. As a result, the drug leakage of the hybrid liposome is restrained significantly at pH 7.4, while at an acidic pH, the drug release is accelerated. The designed pH/temperature dual-sensitive copolymer is expected to provide more precise targeting and environmentally controlled drug release to drug delivery systems based on liposomes.