Design of guaiazulene derivatives-conjugated podophyllotoxin nano-prodrug toward anticancer drug delivery

Kiyotaka Maruoka, Yoshitaka Koseki, Anh Thi Ngoc Dao, Ryuju Suzuki, Anudari Batbayar, Nagaki Sugeno, Hirohito Umezawa, Hitoshi Kasai

Research output: Contribution to journalArticlepeer-review

Abstract

In nanoparticle-based drug delivery systems, dispersion stability is one of the most significant factors controlling drug efficacy and side effects. Herein, we synthesized guaiazulene derivatives-conjugated podophyllotoxin prodrugs and fabricated their nanoparticles (GA-CN-PPT nano-prodrugs). GA-CN-PPT nano-prodrugs were obtained with a size of about 100 nm and possessed high dispersion stability. The cytotoxicity was tunable by changing the length of the carbon chain linker. Notably, the release rate of PPT was the key factor for the anticancer activity of GA-CN-PPT nano-prodrugs. The nano-prodrugs could serve as a promising template for developing a novel delivery system using nano-prodrugs.

Original languageEnglish
JournalMolecular Crystals and Liquid Crystals
DOIs
Publication statusAccepted/In press - 2022

Keywords

  • guaiazulene
  • Nano-prodrugs
  • podophyllotoxin
  • reprecipitation method

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