CIESC Journal ›› 2020, Vol. 71 ›› Issue (10): 4808-4819.doi: 10.11949/0438-1157.20200780

• Material science and engineering, nanotechnology • Previous Articles     Next Articles

Synthesis of PEGylation hydroxyapatite drug delivery system and its dual channels fluorescence imaging

Xiaojing LI(),Wen SUN,Yao KANG,Jiangli FAN(),Xiaojun PENG   

  1. State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024, Liaoning, China
  • Received:2020-06-19 Revised:2020-07-23 Online:2020-10-05 Published:2020-08-10
  • Contact: Jiangli FAN;


PEGylated drug delivery systems (DDSs) can overcome the side effects of traditional chemotherapy by enhancing drug permeability and retention (EPR) effects. In this work, DOX@HAP (hydroxyapatite) was initially fabricated via the coprecipitation and hydrothermal method, further functionalized with Cy (cyanine) by coupling reaction of APTES and then introduced hydrophilic PEG chains by using copper(I)-catalyzed alkyne–azide cycloaddition reaction. Physicochemical properties including the morphology, particle size and phase composition, were characterized by TEM, SEM, particle size analyzer, FTIR, XPS and XRD. The encapsulation efficiency and drug release profile of DOX@HAP-Cy-PEG were analyzed by UV-Vis spectrophotometry. Furthermore, the cellular uptake of DOX@HAP-Cy-PEG nanoparticles in Hela and HepG2 cells was monitored by the dual channels fluorescence imaging of DOX and Cy. The results showed that DOX@HAP-Cy-PEG nanoparticles could be used to real-time monitor the dynamic distribution of DDSs in Hela and HepG2 cells by dual channels.

Key words: hydroxyapatite, drug delivery system, cyanine, dual channels, fluorescence imaging

CLC Number: 

  • TQ 34


Reaction equation of cyanine dyes and PEG alkynyl"


TEM (a) and SEM (b) images of DOX@HAP. DLS analysis (c), zeta potential (d) and PDI values (e) of DOX@HAP,DOX@HAP-Cy and DOX@HAP-Cy-PEG"


XPS (a) and XRD (b) patterns of DOX@HAP. FTIR spectra (c) of HAP,DOX@HAP,DOX@HAP-Cy and DOX@HAP-Cy-PEG"


The absorption spectra (a) and fluorescence spectra (b) of DOX,Cy and DOX@HAP-Cy-PEG"


The absorption spectra of the supernatant liquid of DOX@HAP treated with PBS at pH 3.0 for 24 h(a). The linear relationship between UV absorption (λab = 500 nm) and concentrations of DOX: (A = 16.27C + 0.0476)(b). Release profiles of DOX from DOX@HAP-Cy-PEG in PBS buffer with different pH (5.0,6.5,7.4) in 24 h(c)"


Dose-dependent cytotoxicity of Hela and HepG2 treated with HAP (a),HAP-Cy-PEG (b) and DOX@HAP-Cy-PEG (c) at various concentrations"


CLSM images of Hela and HepG2 cells incubated with DOX@HAP-Cy-PEG for 4 h by dual channels fluorescence imaging"


Synthetic route of PEG-alkyne"


Synthetic route of DOX@HAP-Cy-PEG"


ESI-MS spectrum of compound 4"


1H NMR spectrum of compound 4"


ESI-MS spectrum of Cy"


1H NMR spectrum of Cy"

Table A1

XPS elemental analysis of DOX@HAP"

ElementPeak binding energy/eVContent/%(atom)
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