Abstract
Drug delivery system is simply defined as a technology to precisely control in vivo fate of drugs for achieving optimal therapeutic efficacy. In order to realize this goal, we should elucidate the molecular mechanism of each transport process and understand characteristics of the total body system. Based on these considerations, we have systematically investigated the mechanism of percutaneous drug absorption and in vivo disposition of macromolecules. In the former research, we have succeeded to elucidate action mechanism of absorption enhancers from a physicochemical viewpoint based on a skin diffusion model and demonstrated efficacy of an approach combining prodrug modification and the enhancer. In the latter study, systemic disposition features of macromolecules were explored in relation to their physicochemical and biological properties, and a strategy for designing targeting system was constructed. Novel delivery systems for cell-specific targeting utilizing receptormediated endocytosis are also developed.
