title: A Eu(3+)/Gd(3+)-EDTA-doped structurally controllable hollow mesoporous carbon for improving the oral bioavailability of insoluble drugs and in vivo tracing.
abstract: A structurally controllable fluorescence-labeled hollow mesoporous carbon (HMC) was simply prepared to improve the oral bioavailability of insoluble drugs and further trace their delivery process in vivo. The hollow structure was derived from an inverse replica process using mesoporous silica as a template and the fluorescent label was prepared by doping the carboxylated HMC with a confinement of Eu(3+)/Gd(3+)-EDTA. The physicochemical properties of the composites were systematically characterized by transmission electron microscopy, Fourier transform infrared spectroscopy and photoluminescence spectra tests prior to studying their effects on drug-release behavior and biodistribution. As a result, the thickness of the carrier's shell was adjusted from 70 nm to 130 nm and the maximum drug loading was up to 73.6%. The model drug carvedilol (CAR) showed sustained release behavior compared to CAR commercial capsules, and the dissolution rate slowed down as the shells got thicker. AUC0-48h and Tmax were enlarged 2.2 and 6.5 fold, respectively, which demonstrated that oral bioavailability was successfully improved. Bioimaging tests showed that the novel carbon vehicle had a long residence time in the gastrointestinal tract. In short, the newly designed HMC is a promising drug carrier for both oral bioavailability improvement and in vivo tracing.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, People's Republic of China.
authors.forename: Jia
authors.initials: J
authors.lastname: Liu
authors.forename: Yating
authors.initials: Y
authors.lastname: Zhao
authors.forename: Yu
authors.initials: Y
authors.lastname: Cui
authors.forename: Yang
authors.initials: Y
authors.lastname: Yue
authors.forename: Yikun
authors.initials: Y
authors.lastname: Gao
authors.forename: Qinfu
authors.initials: Q
authors.lastname: Zhao
authors.forename: Jie
authors.initials: J
authors.lastname: Liu
authors.forename: Siling
authors.initials: S
authors.lastname: Wang
mesh_terms: D001682:Biological Availability; D002244:Carbon / Q000737:chemistry*; D004337:Drug Carriers; D004492:Edetic Acid; D005063:Europium; D005682:Gadolinium; D016062:Porosity; D012822:Silicon Dioxide; D012995:Solubility; D014018:Tissue Distribution
chemical_list: D004337:Drug Carriers; D005063:Europium; D002244:Carbon; D012822:Silicon Dioxide; D004492:Edetic Acid; D005682:Gadolinium