Synthesis and characterization of dual-sensitive fluorescent nanogels for enhancing drug delivery and tracking intracellular drug delivery

Szu Yuan Wu, Tilahun Ayane Debele, Yu Chih Kao, Hsieh Chih Tsai

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Here, dual-sensitive fluorescent branched alginate-polyethyleneimine copolymer (bAPSC) nanogels were synthesized from thiolated alginate and stearoyl-derivatized branched polyethyleneimine. The formation of bAPSC conjugates was confirmed through proton nuclear magnetic resonance and Fourier transform infrared spectroscopy, whereas dynamic light scattering was used to measure the particle size and ζ potential of the nanogels. The fluorescent properties of the nanogels were confirmed through fluorescent spectroscopy and microscopy. In addition to the excitation-dependent fluorescence behavior, the fluorescence emission intensity of bAPSC wasaltered by both pH and -irradiation. This intensity was higher at a lower pH than at a higher pH, and it slightly decreased after -irradiation. The drug loading and encapsulation efficiency of bAPSC were 25.9% and 11.2%, respectively. An in vitro drug release study revealed that the synthesized nanogels release their doxorubicin (Dox) contents in a time-dependent manner, and the drug release was higher after 96 h of incubation. Approximately 43.74% and 88.36% of Dox was released after 96 h of incubation at pH 5.5 in the absence and presence of glutathione (GSH), respectively. However, relatively lower drug release, approximately 21.6% and 16%, was observed in the presence and absence of GSH at pH 7.4, respectively. Fluorescence microscopy confirmed that Dox-loaded bAPSC nanogels were internalized by HeLa cells, and drug distribution was easily tracked using fluorescent materials without additional probing agents. Moreover, cellular cytotoxicity and hemolysis results revealed less cytotoxicity and hemocompatibility of the synthesized nanogels, confirming that they are the most favorable alternative drug carriers for drug delivery systems.

Original languageEnglish
Article number1090
JournalInternational Journal of Molecular Sciences
Volume18
Issue number5
DOIs
Publication statusPublished - May 19 2017

Fingerprint

Alginate
Cytotoxicity
Drug delivery
delivery
drugs
Fluorescence
Nuclear magnetic resonance
Irradiation
Fluorescence microscopy
Dynamic light scattering
synthesis
Encapsulation
Pharmaceutical Preparations
Doxorubicin
Fourier transform infrared spectroscopy
Polyethyleneimine
Microscopic examination
Copolymers
Particle size
Spectroscopy

Keywords

  • Alginate
  • Fluorescent organic nanoparticles
  • Nanogel
  • Polyethyleneimine
  • Redox-sensitive

ASJC Scopus subject areas

  • Catalysis
  • Molecular Biology
  • Computer Science Applications
  • Spectroscopy
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

Cite this

Synthesis and characterization of dual-sensitive fluorescent nanogels for enhancing drug delivery and tracking intracellular drug delivery. / Wu, Szu Yuan; Debele, Tilahun Ayane; Kao, Yu Chih; Tsai, Hsieh Chih.

In: International Journal of Molecular Sciences, Vol. 18, No. 5, 1090, 19.05.2017.

Research output: Contribution to journalArticle

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abstract = "Here, dual-sensitive fluorescent branched alginate-polyethyleneimine copolymer (bAPSC) nanogels were synthesized from thiolated alginate and stearoyl-derivatized branched polyethyleneimine. The formation of bAPSC conjugates was confirmed through proton nuclear magnetic resonance and Fourier transform infrared spectroscopy, whereas dynamic light scattering was used to measure the particle size and ζ potential of the nanogels. The fluorescent properties of the nanogels were confirmed through fluorescent spectroscopy and microscopy. In addition to the excitation-dependent fluorescence behavior, the fluorescence emission intensity of bAPSC wasaltered by both pH and -irradiation. This intensity was higher at a lower pH than at a higher pH, and it slightly decreased after -irradiation. The drug loading and encapsulation efficiency of bAPSC were 25.9{\%} and 11.2{\%}, respectively. An in vitro drug release study revealed that the synthesized nanogels release their doxorubicin (Dox) contents in a time-dependent manner, and the drug release was higher after 96 h of incubation. Approximately 43.74{\%} and 88.36{\%} of Dox was released after 96 h of incubation at pH 5.5 in the absence and presence of glutathione (GSH), respectively. However, relatively lower drug release, approximately 21.6{\%} and 16{\%}, was observed in the presence and absence of GSH at pH 7.4, respectively. Fluorescence microscopy confirmed that Dox-loaded bAPSC nanogels were internalized by HeLa cells, and drug distribution was easily tracked using fluorescent materials without additional probing agents. Moreover, cellular cytotoxicity and hemolysis results revealed less cytotoxicity and hemocompatibility of the synthesized nanogels, confirming that they are the most favorable alternative drug carriers for drug delivery systems.",
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AB - Here, dual-sensitive fluorescent branched alginate-polyethyleneimine copolymer (bAPSC) nanogels were synthesized from thiolated alginate and stearoyl-derivatized branched polyethyleneimine. The formation of bAPSC conjugates was confirmed through proton nuclear magnetic resonance and Fourier transform infrared spectroscopy, whereas dynamic light scattering was used to measure the particle size and ζ potential of the nanogels. The fluorescent properties of the nanogels were confirmed through fluorescent spectroscopy and microscopy. In addition to the excitation-dependent fluorescence behavior, the fluorescence emission intensity of bAPSC wasaltered by both pH and -irradiation. This intensity was higher at a lower pH than at a higher pH, and it slightly decreased after -irradiation. The drug loading and encapsulation efficiency of bAPSC were 25.9% and 11.2%, respectively. An in vitro drug release study revealed that the synthesized nanogels release their doxorubicin (Dox) contents in a time-dependent manner, and the drug release was higher after 96 h of incubation. Approximately 43.74% and 88.36% of Dox was released after 96 h of incubation at pH 5.5 in the absence and presence of glutathione (GSH), respectively. However, relatively lower drug release, approximately 21.6% and 16%, was observed in the presence and absence of GSH at pH 7.4, respectively. Fluorescence microscopy confirmed that Dox-loaded bAPSC nanogels were internalized by HeLa cells, and drug distribution was easily tracked using fluorescent materials without additional probing agents. Moreover, cellular cytotoxicity and hemolysis results revealed less cytotoxicity and hemocompatibility of the synthesized nanogels, confirming that they are the most favorable alternative drug carriers for drug delivery systems.

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