Encapsulation of morin in lipid core/PLGA shell nanoparticles significantly enhances its anti-inflammatory activity and oral bioavailability
Morin (3,5,7,2′,4′-pentahydroxyflavone; MR) is a bioactive plant polyphenol whose therapeutic efficacy is hindered by its poor biopharmaceutical properties. The purpose of this study was to develop a nanoparticle (NP) formulation to enhance the bioactivity and oral bioavailability of MR. The nanopre...
| Main Authors: | , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Elsevier
2023-06-01
|
| Series: | Saudi Pharmaceutical Journal |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319016423000920 |
| _version_ | 1797813763517186048 |
|---|---|
| author | Suhair Sunoqrot Malak Alkurdi Abdel Qader Al Bawab Alaa M. Hammad Rabab Tayyem Ali Abu Obeed Mohammed Abufara |
| author_facet | Suhair Sunoqrot Malak Alkurdi Abdel Qader Al Bawab Alaa M. Hammad Rabab Tayyem Ali Abu Obeed Mohammed Abufara |
| author_sort | Suhair Sunoqrot |
| collection | DOAJ |
| description | Morin (3,5,7,2′,4′-pentahydroxyflavone; MR) is a bioactive plant polyphenol whose therapeutic efficacy is hindered by its poor biopharmaceutical properties. The purpose of this study was to develop a nanoparticle (NP) formulation to enhance the bioactivity and oral bioavailability of MR. The nanoprecipitation technique was employed to encapsulate MR in lipid-cored poly(lactide-co-glycolide) (PLGA) NPs. The optimal NPs were about 200 nm in size with an almost neutral surface charge and a loading efficiency of 82%. The NPs exhibited sustained release of MR within 24 h. In vitro antioxidant assays showed that MR encapsulation did not affect its antioxidant activity. On the other hand, anti-inflammatory assays in lipopolysaccharide-stimulated macrophages revealed a superior anti-inflammatory activity of MR NPs compared to free MR. Furthermore, oral administration of MR NPs to mice at a single dose of 20 mg/kg MR achieved a 5.6-fold enhancement in bioavailability and a prolongation of plasma half-life from 0.13 to 0.98 h. The results of this study present a promising NP formulation for MR which can enhance its oral bioavailability and bioactivity for the treatment of different diseases such as inflammation. |
| first_indexed | 2024-03-13T07:57:34Z |
| format | Article |
| id | doaj.art-e0ff0138ea6a4fe89a2e864b9595633f |
| institution | Directory Open Access Journal |
| issn | 1319-0164 |
| language | English |
| last_indexed | 2024-03-13T07:57:34Z |
| publishDate | 2023-06-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Saudi Pharmaceutical Journal |
| spelling | doaj.art-e0ff0138ea6a4fe89a2e864b9595633f2023-06-02T04:22:47ZengElsevierSaudi Pharmaceutical Journal1319-01642023-06-01316845853Encapsulation of morin in lipid core/PLGA shell nanoparticles significantly enhances its anti-inflammatory activity and oral bioavailabilitySuhair Sunoqrot0Malak Alkurdi1Abdel Qader Al Bawab2Alaa M. Hammad3Rabab Tayyem4Ali Abu Obeed5Mohammed Abufara6Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, Jordan; Corresponding author at: Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, P.O. Box 130, Amman 11733, Jordan.Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, JordanDepartment of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, JordanDepartment of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, JordanACDIMA Biocenter, Amman 11190, JordanACDIMA Biocenter, Amman 11190, JordanACDIMA Biocenter, Amman 11190, JordanMorin (3,5,7,2′,4′-pentahydroxyflavone; MR) is a bioactive plant polyphenol whose therapeutic efficacy is hindered by its poor biopharmaceutical properties. The purpose of this study was to develop a nanoparticle (NP) formulation to enhance the bioactivity and oral bioavailability of MR. The nanoprecipitation technique was employed to encapsulate MR in lipid-cored poly(lactide-co-glycolide) (PLGA) NPs. The optimal NPs were about 200 nm in size with an almost neutral surface charge and a loading efficiency of 82%. The NPs exhibited sustained release of MR within 24 h. In vitro antioxidant assays showed that MR encapsulation did not affect its antioxidant activity. On the other hand, anti-inflammatory assays in lipopolysaccharide-stimulated macrophages revealed a superior anti-inflammatory activity of MR NPs compared to free MR. Furthermore, oral administration of MR NPs to mice at a single dose of 20 mg/kg MR achieved a 5.6-fold enhancement in bioavailability and a prolongation of plasma half-life from 0.13 to 0.98 h. The results of this study present a promising NP formulation for MR which can enhance its oral bioavailability and bioactivity for the treatment of different diseases such as inflammation.http://www.sciencedirect.com/science/article/pii/S1319016423000920Anti-inflammatoryBioavailabilityMorinNanoencapsulationPLGA |
| spellingShingle | Suhair Sunoqrot Malak Alkurdi Abdel Qader Al Bawab Alaa M. Hammad Rabab Tayyem Ali Abu Obeed Mohammed Abufara Encapsulation of morin in lipid core/PLGA shell nanoparticles significantly enhances its anti-inflammatory activity and oral bioavailability Saudi Pharmaceutical Journal Anti-inflammatory Bioavailability Morin Nanoencapsulation PLGA |
| title | Encapsulation of morin in lipid core/PLGA shell nanoparticles significantly enhances its anti-inflammatory activity and oral bioavailability |
| title_full | Encapsulation of morin in lipid core/PLGA shell nanoparticles significantly enhances its anti-inflammatory activity and oral bioavailability |
| title_fullStr | Encapsulation of morin in lipid core/PLGA shell nanoparticles significantly enhances its anti-inflammatory activity and oral bioavailability |
| title_full_unstemmed | Encapsulation of morin in lipid core/PLGA shell nanoparticles significantly enhances its anti-inflammatory activity and oral bioavailability |
| title_short | Encapsulation of morin in lipid core/PLGA shell nanoparticles significantly enhances its anti-inflammatory activity and oral bioavailability |
| title_sort | encapsulation of morin in lipid core plga shell nanoparticles significantly enhances its anti inflammatory activity and oral bioavailability |
| topic | Anti-inflammatory Bioavailability Morin Nanoencapsulation PLGA |
| url | http://www.sciencedirect.com/science/article/pii/S1319016423000920 |
| work_keys_str_mv | AT suhairsunoqrot encapsulationofmorininlipidcoreplgashellnanoparticlessignificantlyenhancesitsantiinflammatoryactivityandoralbioavailability AT malakalkurdi encapsulationofmorininlipidcoreplgashellnanoparticlessignificantlyenhancesitsantiinflammatoryactivityandoralbioavailability AT abdelqaderalbawab encapsulationofmorininlipidcoreplgashellnanoparticlessignificantlyenhancesitsantiinflammatoryactivityandoralbioavailability AT alaamhammad encapsulationofmorininlipidcoreplgashellnanoparticlessignificantlyenhancesitsantiinflammatoryactivityandoralbioavailability AT rababtayyem encapsulationofmorininlipidcoreplgashellnanoparticlessignificantlyenhancesitsantiinflammatoryactivityandoralbioavailability AT aliabuobeed encapsulationofmorininlipidcoreplgashellnanoparticlessignificantlyenhancesitsantiinflammatoryactivityandoralbioavailability AT mohammedabufara encapsulationofmorininlipidcoreplgashellnanoparticlessignificantlyenhancesitsantiinflammatoryactivityandoralbioavailability |