@article{065b4826f4b6498797c5a07f8e594935,
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.",
keywords = "beta-casein, bioavailability, celecoxib, micelles",
author = "Hadas Perlstein and Yaelle Bavli and Tanya Turovsky and Abraham Rubinstein and Dganit Danino and David Stepensky and Yechezkel Barenholz",
note = "Funding Information: Acknowledgments: This study was supported in part by a NOFAR grant from the Israel OCS to YB and DD. The authors would like to thank: Dr. Simcha Even-Chen, formerly from the Laboratory of Membrane and Liposome Research, for her help of this research. Dr. Yaron Dagan and Mariana Scherem, of the Authority for Biological and Biomedical Models of the Hebrew University, for their assistance in the pig studies. Dr. Yoav Mintz and David Kushnir, of the Center for Innovative Surgery, Hadassah-Hebrew University Medical Center, for the intraduodenal administrations in the pig studies. Adi Chalilov, formerly from the Technion Department of Biotechnology and Food Engineering, for large-scale preparation of Cx/bCN. Dr. Yael Amir and Amos Avneri, of Euromar Ltd., for supplying the hard gelatin capsules. Mr. Sigmund Geller for editing this manuscript. Publisher Copyright: {\textcopyright} 2014 by De Gruyter 2014.",
year = "2014",
month = dec,
day = "1",
doi = "10.1515/ejnm-2014-0025",
language = "English",
volume = "6",
pages = "217--226",
journal = "European Journal of Nanomedicine",
issn = "1662-5986",
publisher = "Walter de Gruyter GmbH",
number = "4",
}