Asian Journal of Pharmaceutical Sciences (Jul 2020)

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

  • Zhenbao Li,
  • Jiaojiao Zhu,
  • Yongqi Wang,
  • Mei Zhou,
  • Dan Li,
  • Shunzhe Zheng,
  • LiLi Yin,
  • Cong Luo,
  • Huicong Zhang,
  • Lu Zhong,
  • Wei Li,
  • Jian Wang,
  • Shuangying Gui,
  • Biao Cai,
  • Yongjun Wang,
  • Jin Sun

Journal volume & issue
Vol. 15, no. 4
pp. 482 – 491

Abstract

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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.

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