Formulation and Evaluation of Pravastatin Sodium-Loaded PLGA Nanoparticles: In vitro–in vivo Studies Assessment
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,...
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Dove Medical Press
2023-02-01
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| Series: | International Journal of Nanomedicine |
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| Online Access: | https://www.dovepress.com/formulation-and-evaluation-of-pravastatin-sodium-loaded-plga-nanoparti-peer-reviewed-fulltext-article-IJN |
| _version_ | 1811165012481277952 |
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| author | Elsayed SI Girgis GNS El-Dahan MS |
| author_facet | Elsayed SI Girgis GNS El-Dahan MS |
| author_sort | Elsayed SI |
| collection | DOAJ |
| description | 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 |
| first_indexed | 2024-04-10T15:31:46Z |
| format | Article |
| id | doaj.art-e375afdbab254936b308e588d9efb53b |
| institution | Directory Open Access Journal |
| issn | 1178-2013 |
| language | English |
| last_indexed | 2024-04-10T15:31:46Z |
| publishDate | 2023-02-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | International Journal of Nanomedicine |
| spelling | doaj.art-e375afdbab254936b308e588d9efb53b2023-02-13T17:59:03ZengDove Medical PressInternational Journal of Nanomedicine1178-20132023-02-01Volume 1872174281609Formulation and Evaluation of Pravastatin Sodium-Loaded PLGA Nanoparticles: In vitro–in vivo Studies AssessmentElsayed SIGirgis GNSEl-Dahan MSSeham 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 activityhttps://www.dovepress.com/formulation-and-evaluation-of-pravastatin-sodium-loaded-plga-nanoparti-peer-reviewed-fulltext-article-IJNpravastatin sodiumplgananoparticleshypolipidemic and hepatoprotective activity |
| spellingShingle | Elsayed SI Girgis GNS El-Dahan MS Formulation and Evaluation of Pravastatin Sodium-Loaded PLGA Nanoparticles: In vitro–in vivo Studies Assessment International Journal of Nanomedicine pravastatin sodium plga nanoparticles hypolipidemic and hepatoprotective activity |
| title | Formulation and Evaluation of Pravastatin Sodium-Loaded PLGA Nanoparticles: In vitro–in vivo Studies Assessment |
| title_full | Formulation and Evaluation of Pravastatin Sodium-Loaded PLGA Nanoparticles: In vitro–in vivo Studies Assessment |
| title_fullStr | Formulation and Evaluation of Pravastatin Sodium-Loaded PLGA Nanoparticles: In vitro–in vivo Studies Assessment |
| title_full_unstemmed | Formulation and Evaluation of Pravastatin Sodium-Loaded PLGA Nanoparticles: In vitro–in vivo Studies Assessment |
| title_short | Formulation and Evaluation of Pravastatin Sodium-Loaded PLGA Nanoparticles: In vitro–in vivo Studies Assessment |
| title_sort | formulation and evaluation of pravastatin sodium loaded plga nanoparticles in vitro ndash in vivo studies assessment |
| topic | pravastatin sodium plga nanoparticles hypolipidemic and hepatoprotective activity |
| url | https://www.dovepress.com/formulation-and-evaluation-of-pravastatin-sodium-loaded-plga-nanoparti-peer-reviewed-fulltext-article-IJN |
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