Dextran-: G -lauric acid as IKK complex inhibitor carrier

Chao Ming Su, Ching Lin, Chen Yu Huang, Jih Chao Yeh, Tien Yao Tsai, Tzong Rong Ger, Ming Chen Wang, Shyh Liang Lou

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Abstract

Copolymeric micelles made from dextran-g-lauric acid were optimized to carry IκB kinase-β inhibitor, IMD-0354, to form a drug delivery system and to verify the effects on drug loading and encapsulation efficiency. Dextran with different molecular weights was modified by lauric acid via an esterification process between the hydroxyl group of dextran and the carboxyl group of lauric acid. The hydrophilic dextran acts as a framework and lauric acid was grafted to its branches, forming an amphiphilic polymer. Fourier transform infrared spectrometry and 1H nuclear magnetic resonance (NMR) were used to confirm and calculate the grafting percentage of dextran-g-lauric acid. The critical micelle concentration (CMC) values were obtained using ultraviolet-visible spectrophotometry, and particle size was measured using dynamic light scattering and transmission electron microscopy (TEM). The effect of drug-loaded micelles was verified using cell viability and immunofluorescence staining. TEM images indicated that the self-assembled micelles are spherical in shape. The drug loading percentage of micelles was 0.76-4.67%, and the encapsulation efficiency was 15.4-93.75%. Regulating the hydrophilic and hydrophobic fragments of dextran-g-lauric acid changed the particle size, grafting rate, CMC, drug loading, and encapsulation efficiency of the polymer. IMD-0354-loaded micelles showed higher apoptosis expression in melanoma than free IMD-0354. This shows that controlled interactions of hydrophilic and hydrophobic regions on dextran-g-lauric acid may have profound effects on drug delivery for cancer treatment.

Original languageEnglish
Pages (from-to)56247-56255
Number of pages9
JournalRSC Advances
Volume7
Issue number89
DOIs
Publication statusPublished - 2017 Jan 1

All Science Journal Classification (ASJC) codes

  • Chemistry(all)
  • Chemical Engineering(all)

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    Su, C. M., Lin, C., Huang, C. Y., Yeh, J. C., Tsai, T. Y., Ger, T. R., Wang, M. C., & Lou, S. L. (2017). Dextran-: G -lauric acid as IKK complex inhibitor carrier. RSC Advances, 7(89), 56247-56255. https://doi.org/10.1039/c7ra04544a