Materials Science and Engineering: C 2014-12-01

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

Minming Wu, Kai Guo, Hongwei Dong, Rong Zeng, Mei Tu, Jianhao Zhao

Index: Mater. Sci. Eng. C. Mater. Biol. Appl. 45 , 162-9, (2014)

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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 by (1)H and (31)P 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. Copyright © 2014 Elsevier B.V. All rights reserved.