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Beta-casein nanocarriers of celecoxib for improved oral bioavailability

Abstract 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.