TY - JOUR
T1 - Beta-casein nanocarriers of celecoxib for improved oral bioavailability
AU - Perlstein, Hadas
AU - Bavli, Yaelle
AU - Turovsky, Tanya
AU - Rubinstein, Abraham
AU - Danino, Dganit
AU - Stepensky, David
AU - Barenholz, Yechezkel
N1 - Publisher Copyright:
© 2014 by De Gruyter 2014.
PY - 2014/12/1
Y1 - 2014/12/1
N2 - 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.
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.
KW - beta-casein
KW - bioavailability
KW - celecoxib
KW - micelles
UR - http://www.scopus.com/inward/record.url?scp=84917698902&partnerID=8YFLogxK
U2 - 10.1515/ejnm-2014-0025
DO - 10.1515/ejnm-2014-0025
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AN - SCOPUS:84917698902
SN - 1662-5986
VL - 6
SP - 217
EP - 226
JO - European Journal of Nanomedicine
JF - European Journal of Nanomedicine
IS - 4
ER -