In the present study, an icariside II-phospholipid complex was prepared, and its physicochemical properties including UV spectrum, IR spectrum, differential scanning calorimetry (DSC) were tested. Furthermore, the absorption of icariside II and icariside II-phospholipid complex was compared in a Caco-2 cell culture model. The results show that icariside II-phospholipid complex could significantly increase the A-B transport of icariside II (P < 0.01), with A-B Papp of (3.92 +/- 0.50) x 10(-6) cm/s compared to control (2.05 +/- 0.18) x 10(-6) cm/s (increased by 91%). Likewise, the B-A transport of icariside II was significantly enhanced (P < 0.01), with Papp of (15.3 +/- 0.72) x 10(-6) cm/s (control) to (22.4 +/- 1.4) x 10(-6) cm/s (46% increase). Efflux ratio of icariside II decreased by 23.5% after forming icariside II-phospholipid complex. The therefore, it could be concluded that phospholipid complexation can increase the intestinal absorption of icariside II.