| In recent years,mesoporous silica has attracted much attention due to its unique characters,including high specific surface area,large pore volume and good stability.Mesoporous silica have been applied in various fields,including carriers,catalysis,absorption and separation.In this study,Celecoxib（CEL）was used as a model drug,mesoporous silica was evaluated as a drug carrier to investigate its effect on the dissolution of poorly insoluble drugs.There are many methods to synthesize mesoporous silica,and in this study,a time-saving and easy to operate room-temperature synthesizing method was selected.Meanwhile,the products were characterized by Dynamic light scattering,X-ray diffraction,and Transmission electron microscope.Then,the effects of different reactants with different mole ratios on the morphology of mesoporous silica were explored.Finally,the optimal mole ratios of the reactants were determined:the mole ratio of water/ethanol was2.5,the mole ratio of CTAB/TEOS was 0.3,and the mole ratio of NH3/TEOS was 11.The obtained mesoporous silica microspheres（MSM）were spherical and possessed an average diameter of around 1μm.CEL@MSM was prepared using mesoporous silica microspheres loaded with Celecoxib,High performance liquid chromatography,Fourier transform infrared spectroscopy,X-ray diffraction and Differential scanning calorimetry were used for detection,The effects of drug loading method,drug loading time and drug loading ratio on drug loading amount,drug form,dissolution rate and pharmacokinetic behavior in vivo were investigated.The results showed that the drug load of solvent evaporation method was higher than that of solution immersion method.Celecoxib in MSM still exists in an amorphous state when the drug load is 30%,The dissolution rate in each medium increased obviously.A further increase in drug loading would lead to the emergence of crystalline celecoxib in MSM and a corresponding decrease in dissolution rate.SD rats were used to study the pharmacokinetics of CEL@MSM with a drug load of 30%,The results showed that the Cmax and AUC of CEL@MSM were significantly increased compared with celecoxib.These results indicate that mesoporous silica microspheres can improve the dissolution rate and bioavailability of celecoxib in vivo,which can be used to improve the efficacy of insoluble drugs.Physical or chemical modification of mesoporous silica microspheres can regulate drug release behavior,In this study,lipid-coated MSM was prepared by investigating different packaging prescriptions and processes using potential changes and transmission electron microscopy characterization.The results showed that the lipid membrane could be successfully coated on the outer layer of MSM using membrane hydration method with a ratio of MSM to phospholipid 1:2,which can be applied for further drug release and permeability research.. |
