Fabrication of Hinokitiol-modified podophyllotoxin nano-prodrugs having a high drug loading capacity

Keita Tanita, Yoshitaka Koseki, Kazue Shimizu, Hirohito Umezawa, Hitoshi Kasai

Research output: Contribution to journalArticlepeer-review


Nano-prodrug is a nanomedicine developed by the reprecipitation method, which allows nanoparticles to be fabricated by only prodrug molecules without using any nanocarriers. In the present study, we synthesized a heterodimer, composed of hinokitiol and podophyllotoxin (PPT) linked via different linkers of carbon chain length as new prodrug compounds, and fabricated their nano-prodrugs. We found that the longer the carbon chain linker, the smaller the size of nanoparticles, and the lower their cytotoxicity. We concluded that heterodimeric prodrugs can be fabricated into nano-prodrugs without reducing their drug loading capacity, and might eventually serve as a promising template for the development of novel nanomedicine.

Original languageEnglish
Pages (from-to)79-85
Number of pages7
JournalMolecular crystals and liquid crystals
Issue number1
Publication statusPublished - 2020 Jul 23


  • Heterodimeric prodrug
  • Hinokitiol
  • nano-prodrugs
  • podophyllotoxin (PPT)
  • reprecipitation method

ASJC Scopus subject areas

  • Chemistry(all)
  • Materials Science(all)
  • Condensed Matter Physics

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