| Title | In vitro and in vivo evaluation of silybin nanosuspensions for oral and intravenous delivery |
| Authors | Wang, Yancai Zhang, Dianrui Liu, Zhaoping Liu, Guangpu Duan, Cunxian Jia, Lejiao Feng, Feifei Zhang, Xiaoyu Shi, Yanqiu Zhang, Qiang |
| Affiliation | Shandong Univ, Dept Pharmaceut, Coll Pharm, Jinan 250012, Peoples R China. Shandong Univ, Ctr New Drugs Evaluat, Jinan 250012, Peoples R China. Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100083, Peoples R China. |
| Keywords | DISSOLUTION RATE ENHANCEMENT HIGH-PRESSURE HOMOGENIZATION POORLY SOLUBLE DRUGS LIPID NANOPARTICLES CELLULAR UPTAKE CACO-2 CELLS NANOCRYSTALS FORMULATION SOLUBILITY TECHNOLOGY |
| Issue Date | 2010 |
| Publisher | nanotechnology |
| Citation | NANOTECHNOLOGY.2010,21,(15). |
| Abstract | In this study, we evaluate the effect of particle sizes on the physicochemical properties of silybin and identify the influence of silybin nanosuspensions on its permeation across the Caco-2 cell monolayer. In vivo pharmacokinetic evaluation of silybin nanosuspensions was also carried out in beagle dogs. TEM, AFM and SEM analyses revealed the effect of homogenization pressure on particle size and morphology, and confirmed the existence of a surfactant-stabilizer film on the surface of nanoparticles. DSC and XRPD experiments manifested that the crystalline state was maintained as particle size was reduced and the enhanced dissolution property was due to the increased surface area. Nanosuspensions had a significant influence on drug transport across the Caco-2 cell monolayer and the enhanced dissolution velocity was responsible for the increased permeability. A pharmacokinetics study in beagle dogs further confirmed the in vitro results and demonstrated that oral administration of silybin nanosuspensions significantly increase its bioavailability compared to the coarse powder. Nanosuspensions of silybin with smaller particle size reveal a higher potential to increase their oral bioavailability; while for intravenous infusion the lower pressure produced silybin nanosuspensions appeared to maintain a more sustained drug release profile. |
| URI | http://hdl.handle.net/20.500.11897/395768 |
| ISSN | 0957-4484 |
| DOI | 10.1088/0957-4484/21/15/155104 |
| Indexed | SCI(E) EI |
| Appears in Collections: | 药学院 天然药物与仿生药物国家重点实验室 |
