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pH-responsive and CD44-targeting polymer micelles based on CD44p-conjugated amphiphilic block copolymer PEG-b-HES-b-PLA for delivery of emodin to breast cancer cells.

Abstract
Herein, an amphiphilic block copolymer CD44-targeting peptide-conjugated polyethylene glycol-block-hydroxyethyl starch-block-poly (L-lactic acid) (CD44p-conjugated PEG-b-HES-b-PLA) are synthesized, which could self-assemble into the pH-responsive and CD44-targeting polymer micelles against breast cancer cells MDA-MB-231. Emodin (Emo) is a natural anthraquino with pharmacological activities in anti-tumor effects. However, Emo suffers from poor water solubility, low biocompatibility, rapid systemic elimination, and off-target side effects, resulting in unsatisfactory treatment outcomes. Nanotechnology-based drug delivery systems have proven great potential for cancer chemotherapy. The constructed polymeric micelles Emo@CD44p-PM have exhibited an average size of 154.5 ± 0.9 nm characterized by DLS and TEM. Further, the Emo@CD44p-PM have effective Emo-loading capacity, good thermal stability, and pH responsiveness. Intracellular uptake study shows the enhanced cellular internalization of Emo@CD44p-PM due to the increased exposure of CD44p enhances the cellular internalization of Emo@CD44p-PM effectively. Furthermore, thein vitroresults showed Emo@CD44p-PM has been observed good biocompatibility and anti-tumor effects. Therefore, the polymeric micelles Emo@CD44p-PM provide a promising delivery strategy of targeted therapy for breast cancer.
AuthorsKai Cheng, Jie Zhou, Yujie Zhao, Yu Chen, Lan Ming, Da Huang, Rui Yang, Zhenyu Lin, Daozhen Chen
JournalNanotechnology (Nanotechnology) Vol. 33 Issue 27 (Apr 20 2022) ISSN: 1361-6528 [Electronic] England
PMID35313287 (Publication Type: Journal Article)
CopyrightCreative Commons Attribution license.
Chemical References
  • CD44 protein, human
  • Drug Carriers
  • Hyaluronan Receptors
  • Micelles
  • Polyesters
  • Polymers
  • Polyethylene Glycols
  • Emodin
Topics
  • Breast Neoplasms (drug therapy)
  • Cell Line, Tumor
  • Drug Carriers
  • Drug Delivery Systems
  • Emodin
  • Female
  • Humans
  • Hyaluronan Receptors
  • Hydrogen-Ion Concentration
  • Micelles
  • Polyesters
  • Polyethylene Glycols
  • Polymers

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