**3.10 Oral administration of the aqueous dispersions of DHP107**

Even though our oral paclitaxel formulations including DHP107 can be taken *per se*, they can also be mixed with water or taste-masking syrups for administration. To examine how the absorption of paclitaxel changes upon feeding the dispersion, DHP107 was mixed with water or syrup at 3:7 by weight. DHP107 was dispersed spontaneously in water to produce emulsion droplets having average diameter of 6-8 μm. By vortexing the mixture of DHP107 and water or syrup for 1 min, the diameters of emulsion droplets were reduced to 6 (polydispersity = 1) or 3 (polydispersity = 1) μm, respectively. By sonicating DHP107/water mixture at 180 KW for 1 min, we also obtained the dispersion with the oil droplets having 1.4 μm (polydispersity = 1) in diameter.

When the dispersions were orally administered, pharmacokinetic profiles did not change significantly except for the fact that the AUC values were reduced to *ca.* 40 ~ 70 % of the original G2 formulation.

#### **3.11 Antitumor efficacy of DHP107 in experimental animals**

To evaluate the antitumor activity of DHP107 in mice, suspension of NCI-H358 cells was injected subcutaneously to Balb/c athymic mice. All of the mice inoculated with the human non-small cell lung cancer cells developed progressively growing tumors. The mice were administered orally with DHP107 (G2, 50 mg/kg) or intravenously with Taxol® (10 mg/kg) for 5 consecutive days 10 days after the inoculation. The entire tumor tissue was removed surgically after the experiment and photographed as shown in Figure 5A. In the group administered with oral DHP107 and intravenous Taxol®, the tumor size was reduced gradually from *ca*. 100 to 15 ± 3 and 19 ± 5 mm3, respectively, in *ca*. 25 days after the administration of the drug and remained unchanged for the duration of the experiment (Figure 5B). The tumor size data for these two groups were indifferent statistically. In the control group administered orally with the vehicle only, the tumor grew continuously to *ca.* 360 ± 20 mm3 in 45 days.
