Improving oral bioavailability of water-insoluble idebenone with bioadhesive liposomes

The clinical application of water-insoluble idebenone (IDB) is significantly suffering from the poor aqueous solubility in the gastrointestinal (GI) fluids and limited oral bioavailability. Herein, we designed an IDB-loaded bioadhesive liposome based on poly (maleic anhydride-alt-1-octadecene) (PMO) (termed as IBL) to improve the intestinal absorption and oral bioavailability. IBL was nanometer-sized particles with a Z-average diameter of 95.12 nm and IDB exhibited as amorphous or molecular state in the IBL formulation. At 2 h of oral administration, the tissue concentration of IDB in the duodenum, jejunum, and ileum in the IBL treated group was notably improved 2.69-, 3.21- and 3.44- fold over counterpart liposomal formulation of IDB (LI). Moreover, in the IBL treated group, the oral bioavailability of IDB was obviously enhanced 3.79-fold than that in free drug suspension and 2.33-fold when compared to counterpart LI treatment. Therefore, the bioadhesive liposome represents a feasible and elegant strategy to improve the oral absorption of water-insoluble IDB.

Automated summary

This study developed a bioadhesive liposome loaded with water-insoluble idebenone to enhance its intestinal absorption and oral bioavailability, resulting in significantly improved tissue concentrations in the duodenum, jejunum, and ileum as well as enhanced oral bioavailability compared to other formulations.