Abstract
Drug delivery (DD) from water to biomembranes is crucial as a primary step of the bioactivity. The application of highly developed 1H and natural-abundance 13C NMR method to both sides of drugs and membranes is expected to make a significant contribution to advances in the DD study. Taking advantage of the site-selective, noninvasive NMR, we have unambiguously specified the bilayer interface and interior as DD sites on the atomic level. The method can be applied to a variety of drugs including anesthetics, endocrine disruptors, bioactive peptides, and proteins. Dynamic properties of drugs, peptides, and lipid components in membranes have also been monitored by using high power pulsed-field-gradient NMR without labeled nuclei.