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Partic. vol. 37 pp. 64-71 (April 2018)
doi: 10.1016/j.partic.2017.06.008

Dual-function baicalin and baicalin-loaded poly(lactic-co-glycolic acid) nanoparticles: Immune activation of dendritic cells and arrest of the melanoma cell cycle at the G2/M phase

Huimei Wanga, Shulan Hana,b, Lianyan Wangb,*, Tingyuan Yangb, Guifeng Zhangb, Lian Yuc, Yue Zhaod

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    • Baicalin and baicalin-loaded PLGA nanoparticles (PLGA-B) were characterized for bioavailability. • Particle size of PLGA-B prepared was ∼120 nm with a dispersity index of 0.103. • PLGA-B could activate dendritic cells to upregulate expression of their surface marker molecules. • PLGA-B could increase apoptosis of melanoma cells and induce cell-cycle arrest at the G2/M phase.


Accumulating evidence suggests that the flavone glycoside baicalin has immunomodulatory effects and antitumor potential. However, its weak stability in solution, poor absorption, and low bioavailability limit its clinical application. To overcome these disadvantages, we developed baicalin-loaded poly(lactic-co-glycolic acid) nanoparticles (PLGA-B) of small size. Next, we evaluated the dual function of immunotherapy and chemotherapy for PLGA-B using immune-related cells and tumor cells. Results showed that PLGA-B were spherical, with a particle size ∼120 nm and narrow size distribution with an excellent polydispersity index of 0.103. In vitro experiments revealed that baicalin and PLGA-B could activate dendritic cells (DCs) to have higher expression of surface marker molecules and costimulatory molecules than those of control cells. Baicalin and PLGA-B could trigger apoptosis in melanoma (B16) cells via cell-cycle arrest at the G2/M phase. These data suggest that PLGA-B have important roles in activating DCs and killing melanoma cells. Our study could lay a foundation for melanoma treatment through a combined strategy of immunotherapy and chemotherapy.

Graphical abstract


Baicalin; Baicalin-loaded PLGA nanoparticles; Dendritic cells activation; Anti-tumor