Investigations of the gingerol oil colon targeting pellets for the treatment of ulcerative colitis

The clinical treatment of ulcerative colitis (UC) faces great challenges due to lifetime medication. In this study, Gingerol oil was extracted and purified by the process easily scale-up and cost effective, with productivity 2.72 & PLUSMN; 0.38% (w/w, versus crude drugs). The quality control of gingerol oil was fully established by HPLC fingerprint with 4 common peaks identified as 6-gingerol, 8-gingerol, 6-shogaol and 10-gingerol. The similarities of 6 batches of gingerol oil are within 0.931-0.999. The protective effects of gingerol oil are equivalent to or even stronger than that of 6-gingerol on inflammation and oxidative stress of HT-29 cells induced by lipopolysaccharide and H2O2, as well as on UC in mice caused by dextran sulfate sodium salt (DSS). Our research conclusions coincide well with the holistic view of Traditional Chinese Medicine and network pharmacology. The absorption kinetics of gingerol oil were conducted using the in situ intestinal perfusion in rats and comparable absorption were achieved in the jejunum, ileum and colon segments within 2 h. Thus, gingerol oil colon targeting pellets were prepared by extrusion-spherization technique. The cumulative dissolution behaviors and mechanisms were observed and analyzed by fitting to dissolution model. Our studies provided reliable theoretical and experimental support for the gingerol oil as reliable therapeutic choice of UC.

Automated summary

In this study, Gingerol oil was extracted and purified using a scalable and cost-effective process, with a productivity of 2.72±0.38% (w/w). The quality control of gingerol oil was established by HPLC fingerprinting, identifying 6-gingerol, 8-gingerol, 6-shogaol, and 10-gingerol as the major components. Gingerol oil showed protective effects against inflammation and oxidative stress in vitro and colitis in mice. The absorption kinetics of gingerol oil in rats were studied, and colon-targeted pellets were prepared for reliable therapeutic application.