title: The mechanism for increasing the oral bioavailability of poorly water-soluble drugs using uniform mesoporous carbon spheres as a carrier.
abstract: Uniform mesoporous carbon spheres (UMCS) were used as a carrier to improve the bioavailability of the model drug, celecoxib (CEL). Furthermore, we investigated the mechanism responsible for the improved bioavailability of CEL. The association, adhesion and uptake of UMCS by intestinal epithelial cells were studied by transmission electron microscopy (TEM), fluorescence-activated cell sorting (FACS) and laser confocal scanning microscopy (LCSM). UMCS was found to promote cellular uptake of CEL. Drug transport in Caco-2 cell monolayers proved that UMCS can significantly reduce the rate of drug efflux and improve CEL permeability. The dissolution rate of CEL from drug-loaded samples was markedly improved compared with pure crystalline CEL; moreover, oral bioavailability of CEL loaded into UMCS was also markedly improved compared with that of commercially available capsules. UMCS indicates the advantages and potential of this method to achieve improved oral absorption by increasing the dissolution rate, cellular uptake and permeability of the drug.
authors.affiliation: a Department of Life Science and Health , Northeastern University , Shenhe District , Shenyang , Liaoning Province , PR China .
authors.forename: Tianyi
authors.initials: T
authors.lastname: Wang
authors.affiliation: b Shenyang Sunshine Pharmaceutical Co., Ltd, Shenyang Economic and Technological Development Zone , Shenyang , Liaoning Province , PR China , and.
authors.forename: Peng
authors.initials: P
authors.lastname: Zhao
authors.affiliation: c Department of Pharmaceutics , Shenyang Pharmaceutical University , Shenhe District , Shenyang , Liaoning Province , PR China.
authors.forename: Qinfu
authors.initials: Q
authors.lastname: Zhao
authors.affiliation: a Department of Life Science and Health , Northeastern University , Shenhe District , Shenyang , Liaoning Province , PR China .
authors.forename: Bing
authors.initials: B
authors.lastname: Wang
authors.affiliation: c Department of Pharmaceutics , Shenyang Pharmaceutical University , Shenhe District , Shenyang , Liaoning Province , PR China.
authors.forename: Siling
authors.initials: S
authors.lastname: Wang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D018938:Caco-2 Cells; D002152:Calorimetry, Differential Scanning; D002244:Carbon / Q000737:chemistry* / Q000633:toxicity; D000068579:Celecoxib / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D018360:Crystallography, X-Ray; D052246:Cyclooxygenase 2 Inhibitors / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D004285:Dogs; D004337:Drug Carriers; D004339:Drug Compounding; D005434:Flow Cytometry; D006801:Humans; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism*; D018613:Microscopy, Confocal; D046529:Microscopy, Electron, Transmission; D010539:Permeability; D016062:Porosity; D033362:Powder Diffraction; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D004337:Drug Carriers; D002244:Carbon; D000068579:Celecoxib
keywords: Cellular uptake; drug delivery; improved oral bioavailability; mesoporous carbon; permeability