**2.2 Preparation of oral paclitaxel formulations**

The compositions of the oral paclitaxel formulations used in the experiments are summarized in Tables 2 and 3. Paclitaxel formulations with various triglycerides (Table 2) were prepared as follows: Paclitaxel in amorphous form was dissolved completely at 10 mg/ml in mixtures of oils consisting of monoolein, triglycerides and Tween 80 by sonication for 30 s. Some of the oral paclitaxel formulations were semi-solid or solid wax at ambient temperatures with the melting points of 30 ~ 50 C, and therefore had to be warmed before oral feeding.

In Table 3, Paclitaxel, amorphous or crystalline, was dissolved completely in excess amount of methylene chloride and mixed subsequently with tricaprylin. Methylene chloride was evaporated completely to prepare paclitaxel/tricaprylin solution by vacuum evaporation (BUCHI rotavapor R-200, Germany) at 40 C for 1 h. The content of methylene chloride was determined by gas chromatography and was less than 100 ppm in the paclitaxel/tricaprylin solution. Monoolein and Tween 80 were added to the paclitaxel/tricaprylin solution and mixed completely by sonication for 30 s. A formulation that does not contain paclitaxel, eG2, was also prepared for control. The oral paclitaxel formulations were semi-solid wax with the melting temperature of 33 ~ 35 C, and were warmed to body temperature before feeding.

Dispersions of the oral paclitaxel formulations (G8, G9, and G10) were prepared by adding 2.3 times (by volume) of distilled water or syrup to the formulation G2 (also will be referred to as DHP107) and by vortexing or sonicating for 1 min.

#### **2.3 Animals**

Male ICR and Balb/c athymic mice, 7 weeks old, were purchased from Orient Bio Co. (Seoul, Korea) and Japan SLC (Japan), respectively, and maintained 1 week. Animal care and handling followed institutional guidelines (Korea Institute of Science and Technology). Mice were maintained with free access to food and water under a 12-h light/dark cycle.
