Abstract: 

Paclitaxel is a drug for the treatment of ovarian, breast, lung and pancreatic cancers. Due to the low absorption rate when given orally, paclitaxel is sold as an intravenous injection formulation. There are number of reasons for low oral bioavailability for paclitaxel. Two of the most important factors impeding the oral absorption include the low aqueous solubility of paclitaxel and the existence of a protection mechanism in the gastrointestinal tract against toxic chemicals. Oil formulations have been prepared to increase the paclitaxel solubility inside the formulation and when dispersed in an aqueous medium. The formulation is adhesive to the intestinal mucosal surface and has an increased oral bioavailability as a result. One of the formulations, referred as DHP107, was selected as a potential commercial product in 2004. Since then, non-clinical trial and clinical trials phase I, II, and III have been conducted and completed recently. The product will be in Korean market after approval of Korean Food and Drug Administration.  

DHP107 is semi-solid oil composed of monoolein, tricaprylin, polysorbate 80 and paclitaxel. When dispersed in water, it forms a mucoadhesive sponge phase, an irregular analog of the lipid cubic mesophase, evidence by x-ray diffraction and cryo transmission electron microscopy experiments. In an excess amount of water, DHP107 forms micron- and submicron- sized particles after peristalsis.