In vitro release and in vitro–in vivo correlation for silybin meglumine incorporated into hollow-type mesoporous silica nanoparticles

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. CONCLUSION 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.