Indomethacin-loaded redox nanoparticles improve oral bioavailability of indomethacin and suppress its small intestinal inflammation.

BACKGROUND

Continuous administration of low-dose nonsteroidal anti-inflammatory drugs such as indomethacin (IND) is associated with an increased risk of gastrointestinal damage. In this study, the authors developed IND-loaded redox nanoparticles (IND@RNP(O)) with core-shell-type polymeric micelles possessing nitroxide radicals as reactive oxygen species scavengers.

RESULTS

Orally administered IND@RNP(O) significantly accumulated in the intestinal mucosa and improved blood uptake of IND. Because of the reactive oxygen species-scavenging effect, IND@RNP(O) did not cause severe inflammation in the small intestine; this effect sharply contrasted with those of orally administered free-IND and IND-loaded polymeric micelles that do not possess reactive oxygen species scavengers.

CONCLUSION

Oral IND@RNP(O) administration is a useful approach for improving the oral bioavailability of IND and suppressing its adverse effects.