Deoxycholic acid-functionalised nanoparticles for oral delivery of rhein

Rhein (RH) is a candidate for the treatment of kidney diseases. However, clinical application of RH is impeded by low aqueous solubility and oral bioavailability. Deoxycholic acid-conjugated nanoparticles (DNPs) were prepared by ionic interaction for enhancing intestinal absorption by targeting the apical sodium-dependent bile acid transporter in the small intestine. Resultant DNPs showed relatively high entrapment efficiency (90.7 +/- 0.73)% and drug-loading efficiency (6.5 +/- 0.29)% with a particle size of approximately 190 nm and good overall dispersibility. In vitro release of RH from DNPs exhibited sustained and pH-dependent profiles. Cellular uptake and apparent permeability coefficient (P-app) of the DNPs were 3.25and 5.05-fold higher than that of RH suspensions, respectively. An in vivo pharmacokinetic study demonstrated significantly enhanced oral bioavailability of RH when encapsulated in DNPs, with 2.40and 3.33-fold higher C-max and AUC(0-inf) compared to RH suspensions, respectively. DNPs are promising delivery platforms for poorly absorbed drugs by oral administration.

Automated summary

The study focuses on the potential of deoxycholic acid-conjugated nanoparticles (DNPs) in improving the treatment of kidney diseases with RH. Results show that DNPs have high entrapment and drug-loading efficiency, and can significantly enhance the oral bioavailability of RH.