Evaluation of liposomal behavior in the gastrointestinal tract after oral administration using real-time in vivo...

Liposomes are regarded as promising drug carriers for enhancing the pharmacological effects of poorly absorbed drugs, such as peptides, following oral administration. Liposomal surface modifications by mucoadhesive polymers could improve drug absorption through interactions with the mucus layer. The main purpose of this study was to establish a method of monitoring the behavior of liposomes within the body after oral administration, particularly in the gastrointestinal (GI) tract, using a real-time in vivo imaging system (IVIS) to elucidate the behavior of surface-modified liposomes. Indocyanine green (ICG) was used as a near-infrared dye to label chitosan (CS) or glycol CS (GCS)-modified liposomes, and to observe the dynamic behavior of the liposomes in rats by noninvasive IVIS after oral administration. First, we validated IVIS results of the rat abdomens by comparing them to quantitative measurements of ICG fluorescence intensity in tissue homogenates. Nano-sized small unilamellar vesicles were retained longer than micro-sized multilamellar vesicles in the GI tract. Furthermore, surface-modified liposomes showed longer-term retention in the GI tract than unmodified liposomes in fasted rats. Moreover, surface modification by CS or GCS effectively prevented the excretion of liposomes from the GI tract and prolonged retention in fed rats.