title: Oral bioavailability of silymarin formulated as a novel 3-day delivery system based on porous silica nanoparticles.
abstract: The purpose of this study was to develop porous silica nanoparticles (PSNs) as a carrier to improve oral bioavailability of poorly water-soluble drugs, using silymarin as a model. PSNs were synthesized by reverse microemulsion and ultrasonic corrosion methods. A 3-day release formulation consisting of a silymarin solid dispersion, a hydrophilic gel matrix and silymarin-loaded PSNs was prepared. In vitro release studies indicated that both the silymarin-loaded PSNs and the 3-day release formulation showed a typical sustained-release pattern over a long period, about 72 h. The in vivo studies revealed that the 3-day release formulation gave a significantly higher plasma concentration and larger area under the concentration-time curves than commercial tablets when orally administered to beagle dogs. This implies that the prepared 3-day release formulation significantly enhanced the oral bioavailability of silymarin, suggesting that PSNs can be used as promising drug carriers for oral sustained release systems. Thus providing a technically feasible approach for improving the oral bioavailability and long-term efficacy of poorly soluble drugs.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, and Center for Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Jingkou District, Zhenjiang, People's Republic of China.
authors.forename: Xia
authors.initials: X
authors.lastname: Cao
authors.forename: Min
authors.initials: M
authors.lastname: Fu
authors.forename: Liang
authors.initials: L
authors.lastname: Wang
authors.forename: Hongfei
authors.initials: H
authors.lastname: Liu
authors.forename: Wenwen
authors.initials: W
authors.lastname: Deng
authors.forename: Rui
authors.initials: R
authors.lastname: Qu
authors.forename: Weiyan
authors.initials: W
authors.lastname: Su
authors.forename: Yawei
authors.initials: Y
authors.lastname: Wei
authors.forename: Ximing
authors.initials: X
authors.lastname: Xu
authors.forename: Jiangnan
authors.initials: J
authors.lastname: Yu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D003692:Delayed-Action Preparations; D004285:Dogs; D016503:Drug Delivery Systems; D008297:Male; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D033362:Powder Diffraction; D012822:Silicon Dioxide; D012838:Silymarin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
chemical_list: D003692:Delayed-Action Preparations; D012838:Silymarin; D012822:Silicon Dioxide