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In situ apolipoprotein E-enriched corona guides dihydroartemisinin-decorating nanoparticles towards LDLr-mediated tumor-homing chemotherapy.


ABSTRACT: The therapeutic efficiency of active targeting nanoparticulate drug delivery systems (nano-DDS) is highly compromised by the plasma proteins adsorption on nanoparticles (NPs) surface, which significantly hinders cell membrane receptors to recognize the designed ligands, and provokes the off-target toxicity and rapid clearance of NPs in vivo. Herein, we report a novel dihydroartemisinin (DHA)-decorating nano-DDS that in situ specifically recruits endogenous apolipoprotein E (apoE) on the NPs surface. The apoE-anchored corona is able to prolong PLGA-PEG2000-DHA (PPD) NPs circulation capability in blood, facilitate NPs accumulating in tumor cells by the passive enhanced permeability and retention (EPR) effect and low-density lipoprotein receptor (LDLr)-mediated target transport, and ultimately improve the in vivo antitumor activity. Our findings demonstrate that the strategy of in situ regulated apoE-enriched corona ensures NPs an efficient LDLr-mediated tumor-homing chemotherapy.

SUBMITTER: Li Z 

PROVIDER: S-EPMC7486546 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature

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<i>In situ</i> apolipoprotein E-enriched corona guides dihydroartemisinin-decorating nanoparticles towards LDLr-mediated tumor-homing chemotherapy.

Li Zhenbao Z   Zhu Jiaojiao J   Wang Yongqi Y   Zhou Mei M   Li Dan D   Zheng Shunzhe S   Yin LiLi L   Luo Cong C   Zhang Huicong H   Zhong Lu L   Li Wei W   Wang Jian J   Gui Shuangying S   Cai Biao B   Wang Yongjun Y   Sun Jin J  

Asian journal of pharmaceutical sciences 20190705 4


The therapeutic efficiency of active targeting nanoparticulate drug delivery systems (nano-DDS) is highly compromised by the plasma proteins adsorption on nanoparticles (NPs) surface, which significantly hinders cell membrane receptors to recognize the designed ligands, and provokes the off-target toxicity and rapid clearance of NPs <i>in vivo</i>. Herein, we report a novel dihydroartemisinin (DHA)-decorating nano-DDS that <i>in situ</i> specifically recruits endogenous apolipoprotein E (apoE) o  ...[more]

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