In the present study, apigenin loaded lipid nanocapsules (AP-LNC) was prepared with phase inversion method and the formulation was optimized by simplex lattice design experiment with drug loading and encapsulation efficiency as the indexes. The drug loading and encapsulation efficiency of the optimal AP-LNC formulation were 1.26 +/- 0.05% and 95.86 +/- 0.38%, respectively. The drug concentration in the AP-LNC solution was 5.88 mg/mL. The shape of the AP-LNC was spherical with good dispersion. The average particle size and zeta potential of the AP-LNC were 46.1 nm and - 28.18 mV, respectively. The in vitro release experiments showed that the release behavior of AP from LNC fitted the two phase dynamics process. The anti-proliferative activity of the AP-LNC was investigated using the MTT assay, and the results showed AP-LNC could significantly enhance the inhibition rate to HepG2 cell and MCF-7 cell. It could be concluded that LNC was a potential carrier for improving solubility and biological activity of AP.