title: In vitro release and in vitro-in vivo correlation for silybin meglumine incorporated into hollow-type mesoporous silica nanoparticles.
abstract: BACKGROUND
  The purpose of this study was to develop a sustained drug-release model for water-soluble drugs using silica nanoparticles.
  
  
  METHODS
  Hollow-type mesoporous silica nanoparticles (HMSNs) were prepared using Na(2)CO(3) solution as the dissolution medium for the first time. The water-soluble compound, silybin meglumine, was used as the model drug. The Wagner-Nelson method was used to calculate the in vivo absorption fraction.
  
  
  RESULTS
  The results of transmission electron microscopy and nitrogen adsorption revealed that the empty HMSNs had uniformly distributed particles of size 50-100 nm, a spherical appearance, a large specific surface area (385.89 ± 1.12 m(2)/g), and ultralow mean pore size (2.74 nm). The highly porous structure allowed a large drug-loading rate (58.91% ± 0.39%). In 0.08 M Na(2)CO(3) solution, silybin meglumine-loaded HMSNs could achieve highly efficacious and long-term sustained release for 72 hours in vitro. The results of in vitro-in vivo correlation revealed that HMSNs in 0.08 M Na(2)CO(3) solution had a correlation coefficient R(2) value of 0.9931, while those of artificial gastric juice and artificial intestinal juice were only 0.9287 and 0.7689, respectively.
  
  
  CONCLUSIONS
  The findings of in vitro-in vivo correlation indicate that HMSNs together with Na(2)CO(3) solution could achieve an excellent linear relationship between in vitro dissolution and in vivo absorption for 72 hours, leading to a promising model for sustained release of water-soluble drugs.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, People's Republic of China.
authors.forename: Xia
authors.initials: X
authors.lastname: Cao
authors.forename: Wen-Wen
authors.initials: WW
authors.lastname: Deng
authors.forename: Min
authors.initials: M
authors.lastname: Fu
authors.forename: Liang
authors.initials: L
authors.lastname: Wang
authors.forename: Shan-Shan
authors.initials: SS
authors.lastname: Tong
authors.forename: Ya-Wei
authors.initials: YW
authors.lastname: Wei
authors.forename: Ying
authors.initials: Y
authors.lastname: Xu
authors.forename: Wei-Yan
authors.initials: WY
authors.lastname: Su
authors.forename: Xi-Ming
authors.initials: XM
authors.lastname: Xu
authors.forename: Jiang-Nan
authors.initials: JN
authors.lastname: Yu
mesh_terms: D000042:Absorption; D000704:Analysis of Variance; D000818:Animals; D004285:Dogs; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics; D005750:Gastric Juice / Q000378:metabolism; D006863:Hydrogen-Ion Concentration; D016014:Linear Models; D008297:Male; D008536:Meglumine / Q000737:chemistry* / Q000493:pharmacokinetics*; D008954:Models, Biological; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D016062:Porosity; D012822:Silicon Dioxide / Q000737:chemistry*; D000077385:Silybin; D012838:Silymarin / Q000737:chemistry* / Q000493:pharmacokinetics*
chemical_list: D004337:Drug Carriers; D012838:Silymarin; D000077385:Silybin; D008536:Meglumine; D012822:Silicon Dioxide