title: Exploitation of 3D face-centered cubic mesoporous silica as a carrier for a poorly water soluble drug: influence of pore size on release rate.
abstract: The purposes of the present work were to explore the potential application of 3D face-centered cubic mesoporous silica (FMS) with pore size of 16.0nm as a delivery system for poorly soluble drugs and investigate the effect of pore size on the dissolution rate. FMS with different pore sizes (16.0, 6.9 and 3.7nm) was successfully synthesized by using Pluronic block co-polymer F127 as a template and adjusting the reaction temperatures. Celecoxib (CEL), which is a BCS class II drug, was used as a model drug and loaded into FMS with different pore sizes by the solvent deposition method at a drug-silica ratio of 1:4. Characterization using scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transformation infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), nitrogen adsorption, X-ray diffraction (XRD), and differential scanning calorimetry (DSC) was used to systematically investigate the drug loading process. The results obtained showed that CEL was in a non-crystalline state after incorporation of CEL into the pores of FMS-15 with pore size of 16.0nm. In vitro dissolution was carried out to demonstrate the effects of FMS with different pore sizes on the release of CEL. The results obtained indicated that the dissolution rate of CEL from FMS-15 was significantly enhanced compared with pure CEL. This could be explained by supposing that CEL encountered less diffusion resistance and its crystallinity decreased due to the large pore size of 16.0nm and the nanopore channels of FMS-15. Moreover, drug loading and pore size both play an important role in enhancing the dissolution properties for the poorly water-soluble drugs. As the pore size between 3.7 and 16.0nm increased, the dissolution rate of CEL from FMS gradually increased.
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, PR China.
authors.forename: Wenquan
authors.initials: W
authors.lastname: Zhu
authors.forename: Long
authors.initials: L
authors.lastname: Wan
authors.forename: Chen
authors.initials: C
authors.lastname: Zhang
authors.forename: Yikun
authors.initials: Y
authors.lastname: Gao
authors.forename: Xin
authors.initials: X
authors.lastname: Zheng
authors.forename: Tongying
authors.initials: T
authors.lastname: Jiang
authors.forename: Siling
authors.initials: S
authors.lastname: Wang
mesh_terms: D000327:Adsorption; D002152:Calorimetry, Differential Scanning; D000068579:Celecoxib; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D009584:Nitrogen / Q000737:chemistry; D016062:Porosity; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology*; D012822:Silicon Dioxide / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*; D013818:Thermogravimetry; D014867:Water / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D011720:Pyrazoles; D013449:Sulfonamides; D014867:Water; D012822:Silicon Dioxide; D000068579:Celecoxib; D009584:Nitrogen
keywords: 3D face-centered cubic mesoporous silica; Drug delivery system; Improved dissolution; Poorly water soluble drug; Pore size