title: Mesoporous carbon as a novel drug carrier of fenofibrate for enhancement of the dissolution and oral bioavailability.
abstract: The purpose of this study was to develop mesoporous carbon loaded with a poorly watersoluble drug to enhance the drug dissolution and improve the oral bioavailability. Mesoporous carbon was synthesized using Pluronic 127 triblock polymer (F127), TEOS and phenolic resins. Fenofibrate (FFB) was chosen as a model drug and loaded onto mesoporous carbon using three different loading methods involving incipient wetness impregnation, and the solvent and melting methods. The effect of the physical state and the specific surface area were investigated using nitrogen adsorption, transmission electron microscopy (TEM), powder X-ray diffraction (XRD) and differential scanning calorimetry (DSC). It was found that the physicochemical properties of the drug as well as the drug loading methods had critical effects on the drug release rate. In vitro drug release studies showed that incorporation of FFB in mesoporous carbon greatly enhanced the dissolution rate in comparison with that of the pure crystalline drug. Moreover, the oral bioavailability of the drug from mesoporous carbon was higher than that of FFB commercial capsules. Furthermore, mesoporous carbon produced no irritation of the mucosa of the gastrointestinal tract as shown by gastric mucosa irritation test.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang 110016, PR China.
authors.forename: Xia
authors.initials: X
authors.lastname: Niu
authors.forename: Long
authors.initials: L
authors.lastname: Wan
authors.forename: Zhong
authors.initials: Z
authors.lastname: Hou
authors.forename: Tianyi
authors.initials: T
authors.lastname: Wang
authors.forename: Changshan
authors.initials: C
authors.lastname: Sun
authors.forename: Jin
authors.initials: J
authors.lastname: Sun
authors.forename: Peng
authors.initials: P
authors.lastname: Zhao
authors.forename: Tongying
authors.initials: T
authors.lastname: Jiang
authors.forename: Siling
authors.initials: S
authors.lastname: Wang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002244:Carbon / Q000737:chemistry*; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D011345:Fenofibrate / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D005753:Gastric Mucosa / Q000033:anatomy & histology / Q000187:drug effects; D000960:Hypolipidemic Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D008297:Male; D016062:Porosity; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility
chemical_list: D004337:Drug Carriers; D000960:Hypolipidemic Agents; D002244:Carbon; D011345:Fenofibrate