| Summary: | Seham I Elsayed, Germeen N S Girgis, Marwa S El-Dahan Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Dakahlia, EgyptCorrespondence: Seham I Elsayed, Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, El-Gomhoria Street, Mansoura, Dakahlia, Egypt, Tel +201066300417, Fax +20504730097, Email iseham410@mans.edu.egPurpose: Pravastatin sodium (PVS) is a hypolipidemic drug which suffers from extensive first-pass metabolism and short half-life. Poly(d,l-lactide-co-glycolide) (PLGA) is considered a promising carrier to improve its hypolipidemic and hepatoprotective activities.Methods: PVS-loaded PLGA nanoparticles (PVS–PLGA-NPs) were prepared by double emulsion method using a full 32 factorial design. The in vitro release and the physical stability studies of the optimized PVS–PLGA-NPs (F5) were performed. Finally, both hypolipidemic and hepatoprotective activities of the optimized F5 NPs were studied and compared to PVS solution.Results: All the studied physical parameters of the prepared NPs were found in the accepted range. The particle size (PS) ranged from 90 ± 0.125 nm to 179.33 ± 4.509 nm, the poly dispersity index (PDI) ranged from 0.121 ± 0.018 to 0.158 ± 0.014. The optimized NPs (F5) have the highest entrapment efficiency (EE%) (51.7 ± 5%), reasonable PS (168.4 ± 2.506 nm) as well as reasonable zeta potential (ZP) (− 28.3 ± 1.18mv). Solid-state characterization indicated that PVS is well entrapped into NPs. All NPs have distinct spherical shape with smooth surface. The prepared NPs showed a controlled release profile. F5 showed good stability at 4 ± 2°C during the whole storage period of 3 months. In vivo study and histopathological examination indicated that F5 NPs showed significant increase in PVS hypolipidemic as well as hepatoprotective activity compared to PVS solution.Conclusion: The PVS–PLGA-NPs could be considered a promising model to evade the first-pass effect and showed improvement in the hypolipidemic and hepatoprotective activities compared to PVS solution.Keywords: pravastatin sodium, PLGA, nanoparticles, hypolipidemic and hepatoprotective activity
|
|---|