Beta-casein nanocarriers of celecoxib for improved oral bioavailability

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

doi:10.1515/ejnm-2014-0025

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 journal › Article › peer-review

33 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 C_max obtained after administration of Cx/bCN was 2.3-fold higher and the T_max 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 language	English
Pages (from-to)	217-226
Number of pages	10
Journal	European Journal of Nanomedicine
Volume	6
Issue number	4
DOIs	https://doi.org/10.1515/ejnm-2014-0025
State	Published - 1 Dec 2014
Externally published	Yes

Keywords

beta-casein
bioavailability
celecoxib
micelles

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title = "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{\textregistered} 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{\textregistered} 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.",

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AU - Perlstein, Hadas

AU - Bavli, Yaelle

AU - Turovsky, Tanya

AU - Rubinstein, Abraham

AU - Danino, Dganit

AU - Stepensky, David

AU - Barenholz, Yechezkel

PY - 2014/12/1

Y1 - 2014/12/1

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AB - 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.

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Beta-casein nanocarriers of celecoxib for improved oral bioavailability

Abstract

Keywords

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