Studies on the treatment of melanoma with folate acid conjugated dextran and lauryl alcohol loaded with IMD0354

Can Liu, Wei Chen, Zizi Chen, Yu Yan, Qing Wang, Huiqing Xie, Xiang Chen, Aijun Wang, Shijie Tang, Jianda Zhou

Research output: Contribution to journalArticle

1 Scopus citations

Abstract

Background: IMD-0354 is a kind of hydrophobic small molecule inhibitor of IKKβ, which can effectively inhibit the NF-κB pathway. Besides, IMD-0354 can inhibit a variety of tumor cells in culture, but its poor water solubility and low utilization have limited its clinical application. Methods: In this study, IMD-0354 was synthesized through esterifying the folate acid (FA) conjugated dextran (Dex) as well as the lauryl alcohol (LA). Results:The particle (IMD/FA-Dex-LA) size was 212.13±10.62nm, the encapsulation efficiency was 89.27±6.51%, and the drug loading was 4.25±0.42%. Cell viability studies indicated that the IMD/FA-Dex-LA effectively inhibited survival of B16F10 cells in culture. Meanwhile, Western Blotting results showed that the nuclear transport of NF-κB was reduced after blocking the IKK pathway, which would thereby suppress melanoma cell division and proliferation. Moreover, subcutaneous tumor implantation experiment revealed that, the drug-loading complex had an obvious effect on suppressing melanoma cells. Findings of this study demonstrated that the IMD-0354 loaded FA-Dex-LA was more effective than IMD-0354 alone. Conclusion: In summary, FA-Dex-LA has been successfully synthesized in this study, which can serve as a carrier for hydrophobic drug. Further, it is believed the FA-Dex-LA can potentially applied in cancer treatment.

Original languageEnglish (US)
Pages (from-to)4655-4663
Number of pages9
JournalOncoTargets and Therapy
Volume12
DOIs
StatePublished - Jan 1 2019

Keywords

  • Dextran
  • Folate acid
  • IKK inhibitor
  • Lauryl alcohol
  • Melanoma

ASJC Scopus subject areas

  • Oncology
  • Pharmacology (medical)

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