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 watersoluble drugs.