Impact of the amount of PEG on prodrug nanoassemblies for efficient cancer therapy

Yaqiao Li, Lingxiao Li, Qianhui Jin, Tian Liu, Jin Sun, Yongjun Wang, Zhijun Yang, Zhonggui He*, Bingjun Sun*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

PEGylation has been widely used to improve the pharmacokinetic properties of prodrug self-assembled nanoparticles (prodrug-SANPs). However, the impacts of the amount of PEG on the self-assemble stability, cellular uptake, pharmacokinetics, and antitumor efficacy of prodrug-SANPs are still unknown. Herein, selenoether bond bridged docetaxel dimeric prodrug was synthesized as the model prodrug. Five prodrug-SANPs were designed by using different mass ratios of prodrugs to PEG (Wprodrug/WDSPE-mPEG2000 = 10:0, 9:1, 8:2, 7:3 and 6:4), and defined as Pure drug NPs, 9:1NPs, 8:2NPs, 7:3 NPs and 6:4 NPs, respectively. Interestingly, 8:2 NPs formed the most compact nanostructure, thus improving the self-assemble stability and pharmacokinetics behavior. In addition, the difference of these prodrug-SANPs in cellular uptake was investigated, and the influence of PEG on cytotoxicity and antitumor efficacy was also clarified in details. The 8:2 NPs exhibited much better antitumor efficacy than other prodrug-SANPs and even commercial product. Our findings demonstrated the pivotal role of the amount of PEG on prodrug-SANPs.

Original languageEnglish
Pages (from-to)241-252
Number of pages12
JournalAsian Journal of Pharmaceutical Sciences
Volume17
Issue number2
DOIs
Publication statusPublished - Mar 2022

Scopus Subject Areas

  • Pharmacology
  • Pharmaceutical Science

User-Defined Keywords

  • Docetaxel
  • Oxidation responsive
  • PEGylation
  • Prodrug
  • Self-assembly nanoparticles

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