title: Inclusion of celecoxib into fibrous ordered mesoporous carbon for enhanced oral bioavailability and reduced gastric irritancy.
abstract: Fibrous ordered mesoporous carbon (FOMC) was developed as a new drug delivery system for loading an insoluble drug, designed to be orally administered, and then to enhance the drug loading capacity, improve the dissolution rate, enhance the oral bioavailability and reduce the gastric damage. Celecoxib (CEL) was chosen as a model drug. The nanostructures and effect of different pore sizes (4.4-7.0 nm) on drug loading and release properties were studied. The results showed that FOMC has a high drug loading capacity (0.599 g/g, drug weight/carrier weight) and the dissolution rate of CEL from FOMC was much faster than pure crystalline CEL using buffer (pH 6.8) as a dissolution medium. Moreover, the oral bioavailability of CEL loaded into FOMC was significantly improved compared with that of CEL capsules and the gastric damage caused by CEL which was loaded in FOMC was also reduced, demonstrating the protective effect of FOMC.
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, PO Box 23, 103 Wenhua Road, Shenhe District, Shenyang, Liaoning Province 110016, PR China.
authors.forename: Peng
authors.initials: P
authors.lastname: Zhao
authors.forename: Haitao
authors.initials: H
authors.lastname: Jiang
authors.forename: Tongying
authors.initials: T
authors.lastname: Jiang
authors.forename: Zhuangzhi
authors.initials: Z
authors.lastname: Zhi
authors.forename: Chao
authors.initials: C
authors.lastname: Wu
authors.forename: Changshan
authors.initials: C
authors.lastname: Sun
authors.forename: Jinghai
authors.initials: J
authors.lastname: Zhang
authors.forename: Siling
authors.initials: S
authors.lastname: Wang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002214:Capsules / Q000737:chemistry / Q000493:pharmacokinetics; D002244:Carbon / Q000737:chemistry* / Q000493:pharmacokinetics*; D000077482:Carbon Fiber; D000068579:Celecoxib; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods; D005753:Gastric Mucosa / Q000187:drug effects*; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry; D049329:Nanostructures / Q000008:administration & dosage / Q000737:chemistry; D010316:Particle Size; D016062:Porosity; D011720:Pyrazoles / Q000737:chemistry* / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013449:Sulfonamides / Q000737:chemistry* / Q000493:pharmacokinetics*
chemical_list: D002214:Capsules; D000077482:Carbon Fiber; D004337:Drug Carriers; D011720:Pyrazoles; D013449:Sulfonamides; D002244:Carbon; D000068579:Celecoxib