In vitro drug release and biological evaluation of biomimetic polymeric micelles self-assembled from amphiphilic deoxycholic acid-phosphorylcholine-chitosan conjugate

  • Wu M
  • Guo K
  • Dong H
 et al. 
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Abstract

Novel biomimetic amphiphilic chitosan derivative, deoxycholic acid-phosphorylcholine-chitosan conjugate (DCA-PCCs) was synthesized based on the combination of Atherton-Todd reaction for coupling phosphorylcholine (PC) and carbodiimide coupling reaction for linking deoxycholic acid (DCA) to chitosan. The chemical structure of DCA-PCCs was characterized by1H and31P nuclear magnetic resonance (NMR). The self-assembly of DCA-PCCs in water was analyzed by fluorescence measurements, dynamic laser light-scattering (DLS), zeta potential and transmission electron microscopy (TEM) technologies. The results confirmed that the amphiphilic DCA-PCCs can self-assemble to form nanosized spherical micelles with biomimetic PC shell. In vitro biological evaluation revealed that DCA-PCCs micelles had low toxicity against NIH/3T3 mouse embryonic fibroblasts as well as good hemocompatibility. Using quercetin as a hydrophobic model drug, drug loading and release study suggested that biomimetic DCA-PCCs micelles could be used as a promising nanocarrier avoiding unfavorable biological response for hydrophobic drug delivery applications.

Author-supplied keywords

  • Biological evaluation
  • Biomimetic
  • Drug release
  • Phosphorylcholine
  • Polymeric micelles

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Authors

  • Minming Wu

  • Kai Guo

  • Hongwei Dong

  • Rong Zeng

  • Mei Tu

  • Jianhao Zhao

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