Abstract: A composition for delivering lipophilic agents to intestinal mucosa and method of making and use thereof are disclosed. The composition comprises an aqueous solution of one or more short chained C2 to C6 fatty acids, and corresponding salts thereof, and one or more lipophilic agents dissolved in the aqueous solution. Preferably the solution is buffered at a pH of between about 3.5 and 10.5. When the composition is administered to the colon and rectum, the short-chained fatty acids are consumed by the intestinal mucosa thereby forcing said lipophilic agents to enter the mucosal lipophilic cell membrane, thereby protecting the cells from the adverse effects of radiation and chemotherapy.