Beta-casein (bCN) micelles were developed as a platform for improved oral bioavailability (BA) of poorly water-soluble drugs. Here we demonstrate a proof-of-concept using the NSAID celecoxib (Cx) loaded into bCN micelles (Cx/bCN). In a crossover pharmacokinetic (PK) study in pigs (n=4), dosed intraduodenally with either the commercial Cx formulation Celebra® or Cx/bCN, the Cmax obtained after administration of Cx/bCN was 2.3-fold higher and the Tmax was 1.57-fold faster, leading to a 1.76-fold increase in the BA of Cx, compared to the Celebra® formulation. It is suggested that this BA enhancement was caused by improvement of Cx solubility in intestinal fluids by bCN micelles, which maintained their Cx cargo in an amorphous state.
ASJC Scopus subject areas
- Medicine (miscellaneous)
- Biomedical Engineering
- Physical and Theoretical Chemistry