PLGA nanoparticle formulation of RK-33: An RNA helicase inhibitor against DDX3

Guus Martinus Bol, Raheela Khan, Marise Rosa Heerma Van Voss, Saritha Tantravedi, Dorian Korz, Yoshinori Kato, Venu Raman

Research output: Contribution to journalArticlepeer-review

9 Scopus citations


Background: The DDX3 helicase inhibitor RK-33 is a newly developed anticancer agent that showed promising results in preclinical research (Bol et al. EMBO Mol Med, 7(5):648-649, 2015). However, due to the physicochemical and pharmacological characteristics of RK-33, we initiated development of alternative formulations of RK-33 by preparing sustained release nanoparticles that can be administered intravenously. Methods: In this study, RK-33 was encapsulated in poly(lactic-co-glycolic acid) (PLGA), one of the most well-developed biodegradable polymers, using the emulsion solvent evaporation method. Results: Hydrodynamic diameter of RK-33-PLGA nanoparticles was about 245 nm with a negative charge, and RK-33-PLGA nanoparticles had a payload of 1.4 % RK-33. RK-33 was released from the PLGA nanoparticles over 7 days (90 ± 5.7 % released by day 7) and exhibited cytotoxicity to human breast carcinoma MCF-7 cells in a time-dependent manner. Moreover, RK-33-PLGA nanoparticles were well tolerated, and systemic retention of RK-33 was markedly improved in normal mice. Conclusions: PLGA nanoparticles have a potential as a parenteral formulation of RK-33.

Original languageEnglish (US)
Pages (from-to)821-827
Number of pages7
JournalCancer Chemotherapy and Pharmacology
Issue number4
StatePublished - Oct 22 2015


  • DDX3
  • Drug release
  • Nanoparticles
  • PLGA
  • RK-33

ASJC Scopus subject areas

  • Oncology
  • Toxicology
  • Pharmacology
  • Cancer Research
  • Pharmacology (medical)


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