Development and Optimization of <i>Nigella sativa</i> Nanoemulsion Loaded with Pioglitazone for Hypoglycemic Effect
Diabetes mellitus (DM) is a metabolic disorder associated with an increased blood glucose level. The world health burden of DM has increased as a result of numerous causes that necessitates suitable treatment. Pioglitazone (PGZ) is a generally prescribed medication for managing type II diabetes. How...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-07-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/14/15/3021 |
| _version_ | 1797440938391371776 |
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| author | Tamer M. Shehata Mervt M. Almostafa Heba S. Elsewedy |
| author_facet | Tamer M. Shehata Mervt M. Almostafa Heba S. Elsewedy |
| author_sort | Tamer M. Shehata |
| collection | DOAJ |
| description | Diabetes mellitus (DM) is a metabolic disorder associated with an increased blood glucose level. The world health burden of DM has increased as a result of numerous causes that necessitates suitable treatment. Pioglitazone (PGZ) is a generally prescribed medication for managing type II diabetes. However, its low solubility creates complications for its formulation. Therefore, the aim of the current study was to incorporate PGZ into a nanoemulsion (NE) formulation prepared with <i>Nigella sativa</i> oil (NSO) to boost the action of PGZ. To our knowledge, no previous study has addressed the combination and synergistic effect of PGZ and NSO as a hypoglycemic NE formulation intended for oral administration. An experiment was designed to test several PGZ-loaded NE formulations, varying factors such as NSO, surfactant and co-surfactant concentrations. These factors were investigated for their influence on responses including particle size and <i>in vitro</i> release. An optimized PGZ-loaded NE was selected and examined for its morphology, kinetic activity and stability. Further, the anti-diabetic effect of the optimized formulation was evaluated using diabetically induced rats. The optimized formula exhibited a good particle size of 167.1 nm and <i>in vitro</i> release of 89.5%. A kinetic study revealed that the drug release followed the Korsmeyer–Peppas mechanism. Additionally, the PGZ-loaded NE formulation was found to be stable, showing non-significant variation in the evaluated parameters when stored at 4 and 25 °C for a period of 3 months. In vivo investigation of the PGZ-loaded NE formulation showed a significant reduction in blood glucose level, which appeared to be enhanced by the presence of NSO. In conclusion, NS-NE could be a promising nanocarrier for enhancing the hypoglycemic effect of PGZ. |
| first_indexed | 2024-03-09T12:15:40Z |
| format | Article |
| id | doaj.art-3d6a810f2d1f4b92bd1c0e2e3b4eb72d |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-09T12:15:40Z |
| publishDate | 2022-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-3d6a810f2d1f4b92bd1c0e2e3b4eb72d2023-11-30T22:46:17ZengMDPI AGPolymers2073-43602022-07-011415302110.3390/polym14153021Development and Optimization of <i>Nigella sativa</i> Nanoemulsion Loaded with Pioglitazone for Hypoglycemic EffectTamer M. Shehata0Mervt M. Almostafa1Heba S. Elsewedy2Al Bilad Bank Scholarly Chair for Food and Security in Saudi Arabia, The Deanship of Scientific Research, The Vice Presidency for Graduate Studies and Scientific Research, King Faisal University, Alhofuf 36362, Al-Ahsa, Saudi ArabiaAl Bilad Bank Scholarly Chair for Food and Security in Saudi Arabia, The Deanship of Scientific Research, The Vice Presidency for Graduate Studies and Scientific Research, King Faisal University, Alhofuf 36362, Al-Ahsa, Saudi ArabiaAl Bilad Bank Scholarly Chair for Food and Security in Saudi Arabia, The Deanship of Scientific Research, The Vice Presidency for Graduate Studies and Scientific Research, King Faisal University, Alhofuf 36362, Al-Ahsa, Saudi ArabiaDiabetes mellitus (DM) is a metabolic disorder associated with an increased blood glucose level. The world health burden of DM has increased as a result of numerous causes that necessitates suitable treatment. Pioglitazone (PGZ) is a generally prescribed medication for managing type II diabetes. However, its low solubility creates complications for its formulation. Therefore, the aim of the current study was to incorporate PGZ into a nanoemulsion (NE) formulation prepared with <i>Nigella sativa</i> oil (NSO) to boost the action of PGZ. To our knowledge, no previous study has addressed the combination and synergistic effect of PGZ and NSO as a hypoglycemic NE formulation intended for oral administration. An experiment was designed to test several PGZ-loaded NE formulations, varying factors such as NSO, surfactant and co-surfactant concentrations. These factors were investigated for their influence on responses including particle size and <i>in vitro</i> release. An optimized PGZ-loaded NE was selected and examined for its morphology, kinetic activity and stability. Further, the anti-diabetic effect of the optimized formulation was evaluated using diabetically induced rats. The optimized formula exhibited a good particle size of 167.1 nm and <i>in vitro</i> release of 89.5%. A kinetic study revealed that the drug release followed the Korsmeyer–Peppas mechanism. Additionally, the PGZ-loaded NE formulation was found to be stable, showing non-significant variation in the evaluated parameters when stored at 4 and 25 °C for a period of 3 months. In vivo investigation of the PGZ-loaded NE formulation showed a significant reduction in blood glucose level, which appeared to be enhanced by the presence of NSO. In conclusion, NS-NE could be a promising nanocarrier for enhancing the hypoglycemic effect of PGZ.https://www.mdpi.com/2073-4360/14/15/3021diabetesnanoemulsion<i>Nigella sativa</i>pioglitazoneoptimizationhypoglycemia |
| spellingShingle | Tamer M. Shehata Mervt M. Almostafa Heba S. Elsewedy Development and Optimization of <i>Nigella sativa</i> Nanoemulsion Loaded with Pioglitazone for Hypoglycemic Effect Polymers diabetes nanoemulsion <i>Nigella sativa</i> pioglitazone optimization hypoglycemia |
| title | Development and Optimization of <i>Nigella sativa</i> Nanoemulsion Loaded with Pioglitazone for Hypoglycemic Effect |
| title_full | Development and Optimization of <i>Nigella sativa</i> Nanoemulsion Loaded with Pioglitazone for Hypoglycemic Effect |
| title_fullStr | Development and Optimization of <i>Nigella sativa</i> Nanoemulsion Loaded with Pioglitazone for Hypoglycemic Effect |
| title_full_unstemmed | Development and Optimization of <i>Nigella sativa</i> Nanoemulsion Loaded with Pioglitazone for Hypoglycemic Effect |
| title_short | Development and Optimization of <i>Nigella sativa</i> Nanoemulsion Loaded with Pioglitazone for Hypoglycemic Effect |
| title_sort | development and optimization of i nigella sativa i nanoemulsion loaded with pioglitazone for hypoglycemic effect |
| topic | diabetes nanoemulsion <i>Nigella sativa</i> pioglitazone optimization hypoglycemia |
| url | https://www.mdpi.com/2073-4360/14/15/3021 |
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