title: In vitro drug release and biological evaluation of biomimetic polymeric micelles self-assembled from amphiphilic deoxycholic acid-phosphorylcholine-chitosan conjugate.
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.
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China.
authors.forename: Minming
authors.initials: M
authors.lastname: Wu
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China.
authors.forename: Kai
authors.initials: K
authors.lastname: Guo
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China.
authors.forename: Hongwei
authors.initials: H
authors.lastname: Dong
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China. Electronic address: tzengronga@jnu.edu.cn.
authors.forename: Rong
authors.initials: R
authors.lastname: Zeng
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China.
authors.forename: Mei
authors.initials: M
authors.lastname: Tu
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China.
authors.forename: Jianhao
authors.initials: J
authors.lastname: Zhao
mesh_terms: D000818:Animals; D040761:Biomimetic Materials / Q000737:chemistry*; D002470:Cell Survival / Q000187:drug effects; D048271:Chitosan / Q000737:chemistry*; D003840:Deoxycholic Acid / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D004912:Erythrocytes / Q000166:cytology / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D051379:Mice; D008823:Micelles; D041681:NIH 3T3 Cells; D010316:Particle Size; D010767:Phosphorylcholine / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry; D011794:Quercetin / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity; D011817:Rabbits; D013050:Spectrometry, Fluorescence
chemical_list: D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; D003840:Deoxycholic Acid; D010767:Phosphorylcholine; D048271:Chitosan; D011794:Quercetin
keywords: Biological evaluation; Biomimetic; Drug release; Phosphorylcholine; Polymeric micelles