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

Authors Liu C, Chen W, Chen Z, Yan Y, Wang Q, Xie H, Chen X, Wang A, Tang S, Zhou J

Received 5 March 2019

Accepted for publication 27 April 2019

Published 14 June 2019 Volume 2019:12 Pages 4655—4663


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 2

Editor who approved publication: Dr Tohru Yamada

Can Liu,1 Wei Chen,2 Zizi Chen,1 Yu Yan,3 Qing Wang,4 Huiqing Xie,5 Xiang Chen,6 Aijun Wang,7 Shijie Tang,8 Jianda Zhou1

1The Third Xiangya Hospital, Central South University, Changsha, Hunan 410013, People’s Republic of China; 2The Xiangya Hospital, Central South University, Changsha, Hunan 410008, People’s Republic of China; 3Xiangya School of Medicine, Central South University, Changsha, Hunan 410013, People’s Republic of China; 4National Institute of Environmental Health, Chinese Center for Disease Control and Prevention, Beijing 102206, People’s Republic of China; 5Department of Rehabilitation, The Third Xiangya Hospital, Central South University, Changsha, Hunan, 410013, People’s Republic of China; 6Department of Dermatology, The Xiangya Hospital, Central South University, Changsha, Hunan, 410008, People’s Republic of China; 7Surgical Bioengeneering Laboratory, School of Medicine, The University of California Davis, Sacramento, CA, 95817, USA; 8Cleft Lip and Palate Treatment Center, The Second Affliated Hospital, Shantou University Medical College, Shantou, Guangdong, 515041, People’s Republic of China

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.

Keywords: dextran, lauryl alcohol, folate acid, IKK inhibitor, melanoma

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