The potential application of strategic released apigenin from polymeric carrier in pulmonary fibrosis

ABSTRACT

Aim: The capability of reducing fibrotic and inflammatory responses in lung tissues represents a gold standard for evaluating the efficacy of therapeutic interventions for treating idiopathic pulmonary fibrosis (IPF). A wide variety of therapeutic strategies have been employed in clinic to treat PF, but limited success has been obtained. Apigenin (4, 5, 7-trihydroxyflavone) is a member of flavonoid family that exerts anti-inflammatory and anti-fibrosis effects. In this study, we explore the potential therapeutic effect of apigenin in lung fibrosis. Materials and Methods: Apigenin was employed to treat IPF in a bleomycin-induced PF rat model. Apigenin was loaded onto a biodegradable polymer carrier (nanoparticle, NP) to improve its bio-solubility and bio-availability. The properties (e.g. size, apigenin loading and release profile) of the apigenin loaded polymer carrier were well-characterized. In vitro study was performed to assess the impact of apigenin on pulmonary cell viability, growth, as well as inflammatory and pro-fibrosis responses in pulmonary cells. The impact of apigenin on the production of inflammatory cytokines (e.g. TGF-β, TNF-α) and pro-fibrosis factors in bronchoalveolar lavage fluid and pulmonary cells from lung tissues was also investigated. Results: Our results showed, apigenin has anti-fibrosis effect by inhibition fibrosis related cytokines expression. And compared with apigenin in soluble form, the strategic release of apigenin is more effective in inhibiting pulmonary fibrosis and inflammation. Conclusion: Our finding suggested that apigenin loaded on polymeric carrier might be an effective treatment for pulmonary fibrosis patients.

KEYWORDS:

• Apigenin
• polymer carrier
• idiopathic pulmonary fibrosis (IPF)

Conflict of interest

The authors declare no conflict of interest.

Funding sources

This research was supported by the following funding sources: Henan science foundation (Grant NO. 142102310504); Department of Transnational Medicines for Key Herb Study (Grant NO. 2013ZY04028), Frontier research support by Department of Science and Technology in Henan province (Grant NO. 112300410052), New Faculty Research Funding Support from Henan University of Traditional Chinese Medicine.