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Celecoxib confinement within mesoporous silicon for enhanced oral bioavailability

100%

Wang F., Barnes T. J., Prestidge C. A.

Mesoporous Biomaterials

2014

vol. 1

issue 1

We investigate the physicochemical characteristics of celecoxib (CEL) entrapped within particles of an oxidized porous silicon matrix (pSiox); determine the oral dose response of CEL compared to pure drug and innovator formulation; develop in vivo-in vitro correlation (IVIVC). CEL was loaded into a pSiox matrix by solvent partitioning, with the physical state of the CEL characterized by FTIR, DSC, TGA and XRD, and correlated with in vitro dissolution behavior. Single dose pharmacokinetic parameters of orally dosed CEL were determined in fasted rats for aqueous suspensions of pure CEL, Celebrexr and CEL-pSiox microparticles. Physicochemical testing of CEL-pSiox formulation confirmed the entrapment of CEL within porous nanostructure in an amorphous or non-crystalline form. CEL-pSiox demonstrated superior pharmacokinetics compared with CEL particles or Celebrexr, i.e. increased absolute bioavailability (96.2% vs. 65.2% vs. 88.1%), increased Cmax (0.91 ± 0.09 μg/mL vs. 0.50 ± 0.16 μg/mL vs. 0.73 ± 0.23 μg/mL) and reduced Tmax (1.0 ± 0.0 h vs. 2.8 ± 0.8 h vs. 3.4 ± 1.0 h). Single point correlation was established between in vitro dissolution efficiency (% DE) and in vivo absolute bioavailability or Cmax . Porous silicon microparticles can be formulated as an effective orally dosed solid dispersion preparation for celecoxib

Celecoxib - A Selective Cyclooxygenase-2 Inhibitor Exhibits Dose - Dependent Chemopreventive Activity on an Animal Model of Colorectal Cancer*

86%

Spychalski M., Dziki Ł., Buczyński J., Kulig A., Sporny S., Dziki A.

Polish Journal of Surgery

2008

vol. 80

issue 5

248-255

Colorectal cancer (CRC) is still one of the unresolved issues in medicine. Despite constant improvements in diagnosis and treatment, the prognosis for CRC is unsatisfactory. In recent years, much attention has been paid to experiments concerning chemoprevention of CRC.The aim of the study was evaluation of the effectiveness of celecoxib, a selective Cyclooxygenase-2 (COX-2) inhibitor of chemically-induced CRC carcinogenesis in Fisher F344 rats.Material and methods. Forty-five four-week old male F344 rats were randomized into four groups. In Groups 1, 2, and 3, we induced the CRC carcinogenesis through two subcutaneous injections of Azoxymethane in doses of 20 mg/kg. Rats from groups 1 and 2 were treated with celecoxib in doses of 10 and 30 mg/kg from the start of the experiment. Group 4 was a negative control. The experiment ended in the 26th week. We assessed the following parameters: the number of Aberrant Crypt Foci (premalignant lesions in colons) and the immunoexpression indexes: COX-2, Vascular Endothelial Growth Factor (VEGF), and c-myc.Results. Celecoxib reduced the ACF number. The ACF reduction was dose-dependent. The median ACF number per field of vision was as follows for each of the groups: 1.7, 0.75, 3.2, and 0.2. Celecoxib, irrespective of the dose, reduced the VEGF immunoexpression index. We did not observe a reduction of COX-2 or c-myc immunoexpression in the celecoxib groups.Conclusions. In this experiment, we proved that celecoxib possessed chemopreventive activity. Carcinogenesis inhibition by selective COX-2 inhibitor was dose-dependent. We demonstrated that celecoxib hidners angiogenesis, expressed as VEGF immunoexpression. We indirectly confirmed the hypothesis of a celecoxib COX-2 independent pathway mechanism of action.

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1 Mesoporous Biomaterials

1 Polish Journal of Surgery

1 2014

1 2008

1 Barnes T. J.

1 Buczyński J.

1 Dziki A.

1 Dziki Ł.

1 Kulig A.

1 Prestidge C. A.

1 Sporny S.

1 Spychalski M.

1 Wang F.

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Celecoxib confinement within mesoporous silicon for enhanced oral bioavailability

Celecoxib - A Selective Cyclooxygenase-2 Inhibitor Exhibits Dose - Dependent Chemopreventive Activity on an Animal Model of Colorectal Cancer*