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Development of a tin oxide carrier with mesoporous structure for improving the dissolution rate and oral relative bioavailability of fenofibrate.
- Source :
-
Drug design, development and therapy [Drug Des Devel Ther] 2018 Jul 10; Vol. 12, pp. 2129-2138. Date of Electronic Publication: 2018 Jul 10 (Print Publication: 2018). - Publication Year :
- 2018
-
Abstract
- Background: Biopharmaceutics classification system class II drugs have low solubility, which limits their extent and speed of absorption after oral administration. Over the years, mesoporous materials have been widely used to increase the dissolution rate and oral relative bioavailability of poorly water-soluble drugs.<br />Objectives: In order to improve the dissolution rate and increase oral relative bioavailability of the poorly water-soluble drugs, a tin oxide carrier (MSn) with a mesoporous structure was successfully synthesized.<br />Methods: In this study, MSn was synthesized using mesoporous silica material (SBA-15) as the template. Fenofibrate (FNB) was adsorbed into the channels of MSn by an adsorption method. Characterizations of the pure FNB, MSn, physical mixture of the drug and MSn (PM; 1:1) and FNB-loaded MSn (FNB-MSn) samples were carried out by the scanning electron microscopy (SEM), transmission electron microscopy (TEM), N <subscript>2</subscript> adsorption/desorption, powder X-ray diffractometer (PXRD), differential scanning calorimetry (DSC) and Fourier transform infrared (FT-IR) spectroscopy. Cytotoxicity assay (MTT) was used to evaluate the cytotoxicity of MSn. In vitro dissolution studies were performed to investigate the dissolution rate of FNB-MSn. In vivo pharmacokinetic studies were used to investigate the changes of plasma drug concentrations of FNB-MSn tablets and commercial FNB tablets in rabbits.<br />Results: Detailed characterization showed that FNB in the channels of MSn was present in an amorphous state. The in vitro release tests demonstrated that MSn with a good biocompatibility could effectively enhance the dissolution rate of FNB. Pharmacokinetic results indicated that MSn significantly increased the oral relative bioavailability of FNB.<br />Conclusion: MSn can be regarded as a promising carrier for an oral drug delivery system.<br />Competing Interests: Disclosure The authors report no conflicts of interest in this work.
- Subjects :
- Administration, Oral
Animals
Biological Availability
Caco-2 Cells
Drug Carriers chemical synthesis
Drug Carriers chemistry
Fenofibrate administration & dosage
Humans
Particle Size
Porosity
Rabbits
Solubility
Surface Properties
Tin Compounds chemical synthesis
Fenofibrate chemistry
Fenofibrate pharmacokinetics
Tin Compounds chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1177-8881
- Volume :
- 12
- Database :
- MEDLINE
- Journal :
- Drug design, development and therapy
- Publication Type :
- Academic Journal
- Accession number :
- 30022811
- Full Text :
- https://doi.org/10.2147/DDDT.S166989