Beta-casein nanocarriers of celecoxib for improved oral bioavailability

Hadas Perlstein, Yaelle Bavli, Tanya Turovsky, Abraham Rubinstein, Dganit Danino, David Stepensky, Yechezkel Barenholz*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

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.

Original languageEnglish
Pages (from-to)217-226
Number of pages10
JournalEuropean Journal of Nanomedicine
Volume6
Issue number4
DOIs
StatePublished - 1 Dec 2014
Externally publishedYes

Keywords

  • beta-casein
  • bioavailability
  • celecoxib
  • micelles

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