Enhanced oral bioavailability of fluvastatin by using nanosuspensions containing cyclodextrin
Enhanced oral bioavailability of fluvastatin by using nanosuspensions containing cyclodextrin
Blog Article
Li Originals Crewneck Sweater Jun,1,2,* Yang Min,2,* Xu Wen-Rong11School of Medical Science and Laboratory Medicine, Jiangsu University, Zhenjiang, Jiangsu 212013, China; 2Department of Intensive Care Unit, Chest Hospital Affiliated to Shanghai Jiaotong University, Shanghai 200030, China*These authors contributed equally to this workBackground: In this study, fluvastatin (FVT) nanosuspensions containing cyclodextrin were developed to improve oral bioavailability.Methods: FVT nanosuspensions containing cyclodextrin were prepared by a high pressure homogenization technique.The nanosuspensions system was then characterized by transmission electron microscopy (TEM), particle size, differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD).In addition, in vitro drug release properties, pharmacokinetics and pharmacodynamics were also investigated in detail.
Results: After lyophilization, the nanosuspensions could be redispersed gently and with a narrow particle size distribution, but the particle size has no obvious change.The powder X-ray diffraction and differential scanning calorimetry of FVT nanosuspensions showed that FVT existed in amorphous form in nanosuspensions.In vitro release, FVT nanosuspensions have sustained-release properties.Meanwhile, FVT nanosuspensions could significantly modify the pharmacokinetic profile and increase the bioavailability of FVT by more than Drone 2.
4-fold in comparison with the FVT capsules group.In vivo irritation test showed that there was almost no evidence of hemorrhagic mucosal erosion and intestinal villus destruction in rat gastric mucosa.Conclusion: The combination of nanocrystallization and cyclodextrin complexation techniques is a new attempt to formulate poorly water-soluble FVT.Keywords: fluvastatin, HP-β-CD, nanosuspensions, bioavailability, irritation test .