Nanoparticle-encapsulated baicalein markedly modulates pro-inflammatory response in gingival epithelial cells

Nanoscale. 2017 Sep 14;9(35):12897-12907. doi: 10.1039/c7nr02546g.


Severe gum disease (periodontitis), which is one of the major global oral diseases, results from microbe-host dysbiosis and dysregulated immuno-inflammatory responses. It seriously affects oral health and general wellbeing with significant socio-economic implications. It has been well documented that natural flavonoids such as baicalin (BA) and baicalein (BE) possess potent anti-inflammatory effects. However, their intrinsic poor solubility and low bioavailability severely limit their biomedical applications. In the present study, BA and BE were encapsulated in our synthesized and amine-modified mesoporous silica nanoparticles (MSNs) (Nano-BA and Nano-BE, respectively), and their loading efficiencies and releasing profiles were investigated. Their cytotoxicity was examined on primary human gingival epithelial cells (hGECs), and the cellular uptake of Nano-BA or Nano-BE was visualized via a transmission electron microscope. Their anti-inflammatory effects were evaluated in IL-1β-treated hGECs using the cytokine array and enzyme-linked immunosorbent assay. The present study shows that the amine-modified MSNs could encapsulate BA and BE, and nano-encapsulation greatly enhances the drug delivery rate and prolongs the release of BA and BE up to 216 h. Moreover, both Nano-BA and Nano-BE could be internalized by hGECs and retained intracellularly in nanoparticle-free media for at least 24 h. Note that Nano-BE pre-treatment effectively down-regulates the IL-1β-induced expression of IL-6 and IL-8 in hGECs. In conclusion, nanoparticle-encapsulated BE exhibits notable anti-inflammatory effects through effective release and cellular internalization approaches. This study may facilitate the development of novel drug delivery systems for improving oral care.

MeSH terms

  • Anti-Inflammatory Agents / administration & dosage*
  • Cells, Cultured
  • Drug Delivery Systems
  • Epithelial Cells / immunology*
  • Flavanones / administration & dosage*
  • Flavonoids / administration & dosage
  • Gingiva / cytology*
  • Humans
  • Inflammation
  • Interleukin-6 / immunology
  • Interleukin-8 / immunology
  • Nanoparticles*


  • Anti-Inflammatory Agents
  • CXCL8 protein, human
  • Flavanones
  • Flavonoids
  • IL6 protein, human
  • Interleukin-6
  • Interleukin-8
  • baicalin
  • baicalein