pH-responsive Polymersome Based on PMCP-<italic style="font-style: italic">b</italic>-PDPA as a Drug Delivery System to Enhance Cellular Internalization and Intracellular Drug Release

Wen-liang Wang; Xiao-jing Ma; Xi-fei Yu

doi:10.1007/s10118-017-1982-x

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pH-responsive Polymersome Based on PMCP-b-PDPA as a Drug Delivery System to Enhance Cellular Internalization and Intracellular Drug Release

Papers | Updated：2021-02-18

- pH-responsive Polymersome Based on PMCP-b-PDPA as a Drug Delivery System to Enhance Cellular Internalization and Intracellular Drug Release
- Chinese Journal of Polymer Science Vol. 35, Issue 11, Pages: 1352-1362(2017)
- Affiliations：
  
  a.The Polymer Composites Engineering Laboratory, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China
  b.University of Science and Technology of China, Hefei 230026, China
- Author bio：
  
  Xiao-jing Ma(马晓晶), E-mail:xjma@ciac.ac.cn
  Xi-fei Yu(于喜飞), E-mail:xfyu@ciac.ac.cn
- Funds：
- DOI：10.1007/s10118-017-1982-x
  CLC：
- Received：31 March 2017，
  
  Revised：2017-5-13，
  
  Accepted：17 May 2017，
  
  Published：05 November 2017
- Accepted：
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Wen-liang Wang, Xiao-jing Ma, Xi-fei Yu. pH-responsive Polymersome Based on PMCP-b-PDPA as a Drug Delivery System to Enhance Cellular Internalization and Intracellular Drug Release[J]. Chinese Journal of Polymer Science, 2017, 35(11): 1352-1362. DOI: 10.1007/s10118-017-1982-x.
DOI：

Wen-liang Wang, Xiao-jing Ma, Xi-fei Yu. pH-responsive Polymersome Based on PMCP-b-PDPA as a Drug Delivery System to Enhance Cellular Internalization and Intracellular Drug Release[J]. Chinese Journal of Polymer Science, 2017, 35(11): 1352-1362. DOI: 10.1007/s10118-017-1982-x. DOI：

摘要

Abstract

Choline phosphate (CP) as a novel zwitterion possesses specific and excellent properties compared with phosphorylcholine (PC)

as well as its polymer

such as poly(2-(methacryloyloxy)ethyl choline phosphate) (PMCP)

has been studied extensively due to its unique characteristics of rapid cellular internalization

via

the special quadrupole interactions with the cell membrane. Recently

we reported a novel PMCP-based drug delivery system to enhance the cellular internalization where the drug was conjugated to the polymer

via

reversible acylhydrazone bond. Herein

to make full use of this feature of PMCP

we synthesized the diblock copolymer poly(2-(methacryloyloxy)ethyl choline phosphate)-

-poly(2-(diisopropylamino)ethyl methacrylate) (PMCP-

-PDPA)

which could self-assemble into polymersomes with hydrophilic PMCP corona and hydrophobic membrane wall in mild conditions when the pH value is ≥ 6.4. It has been found that these polymersomes can be successfully used to load anticancer drug Dox with the loading content of about 11.30 wt%. After the polymersome is rapidly internalized by the cell with the aid of PMCP

the loaded drug can be burst-released in endosomes since PDPA segment is protonated at low pH environment

which renders PDPA to transfer from hydrophobic to hydrophilic

and the subsequent polymersomes collapse thoroughly. Ultimately

the "proton sponge" effect of PDPA chain can further accelerate the Dox to escape from endosome to cytoplasm to exert cytostatic effects. Meanwhile

the cell viability assays showed that the Dox-loaded polymersomes exhibited significant inhibitory effect on tumor cells

indicating its great potential as a targeted intracellular delivery system with high efficiency.

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pH-responsive Polymersome Based on PMCP-b-PDPA as a Drug Delivery System to Enhance Cellular Internalization and Intracellular Drug Release

DOI：10.1007/s10118-017-1982-x

摘要

Abstract

关键词

Keywords

references