Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation
Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and t...
| Main Authors: | , , , , , , , , , , , , |
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| Format: | Article |
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MDPI AG
2021-10-01
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| Series: | Nanomaterials |
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| Online Access: | https://www.mdpi.com/2079-4991/11/11/2920 |
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| author | Ameeduzzafar Zafar Syed Sarim Imam Nabil K. Alruwaili Omar Awad Alsaidan Mohammed H. Elkomy Mohammed M. Ghoneim Sultan Alshehri Ahmed Mahmoud Abdelhaleem Ali Khalid Saad Alharbi Mohd Yasir Kaveripakkam M. Noorulla Sami I. Alzarea Abdullah S. Alanazi |
| author_facet | Ameeduzzafar Zafar Syed Sarim Imam Nabil K. Alruwaili Omar Awad Alsaidan Mohammed H. Elkomy Mohammed M. Ghoneim Sultan Alshehri Ahmed Mahmoud Abdelhaleem Ali Khalid Saad Alharbi Mohd Yasir Kaveripakkam M. Noorulla Sami I. Alzarea Abdullah S. Alanazi |
| author_sort | Ameeduzzafar Zafar |
| collection | DOAJ |
| description | Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (<i>p</i> < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against <i>S. aureus</i> and <i>P. aeruginosa</i> and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (<i>p</i> < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity. |
| first_indexed | 2024-03-10T05:12:58Z |
| format | Article |
| id | doaj.art-8140c9b4db6f448683e47472324060ea |
| institution | Directory Open Access Journal |
| issn | 2079-4991 |
| language | English |
| last_indexed | 2024-03-10T05:12:58Z |
| publishDate | 2021-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Nanomaterials |
| spelling | doaj.art-8140c9b4db6f448683e47472324060ea2023-11-23T00:40:25ZengMDPI AGNanomaterials2079-49912021-10-011111292010.3390/nano11112920Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo EvaluationAmeeduzzafar Zafar0Syed Sarim Imam1Nabil K. Alruwaili2Omar Awad Alsaidan3Mohammed H. Elkomy4Mohammed M. Ghoneim5Sultan Alshehri6Ahmed Mahmoud Abdelhaleem Ali7Khalid Saad Alharbi8Mohd Yasir9Kaveripakkam M. Noorulla10Sami I. Alzarea11Abdullah S. Alanazi12Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi ArabiaDepartment of Pharmacy Practice, College of Pharmacy, AlMaarefa University, Ad Diriyah 13713, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics and Industrial Pharmacy, College of Pharmacy, Taif University, Taif 21944, Saudi ArabiaDepartment of Pharmacology, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi ArabiaDepartment of Pharmacy, College of Health Sciences, Arsi University, Asella P.O. Box 396, EthiopiaDepartment of Pharmacy, College of Health Sciences, Arsi University, Asella P.O. Box 396, EthiopiaDepartment of Pharmacology, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi ArabiaDepartment of Clinical Pharmacy, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi ArabiaHypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (<i>p</i> < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against <i>S. aureus</i> and <i>P. aeruginosa</i> and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (<i>p</i> < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.https://www.mdpi.com/2079-4991/11/11/2920oral deliverypiperinesolid self nanoemusifyingantimicrobial activityantihypertensive activity |
| spellingShingle | Ameeduzzafar Zafar Syed Sarim Imam Nabil K. Alruwaili Omar Awad Alsaidan Mohammed H. Elkomy Mohammed M. Ghoneim Sultan Alshehri Ahmed Mahmoud Abdelhaleem Ali Khalid Saad Alharbi Mohd Yasir Kaveripakkam M. Noorulla Sami I. Alzarea Abdullah S. Alanazi Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation Nanomaterials oral delivery piperine solid self nanoemusifying antimicrobial activity antihypertensive activity |
| title | Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation |
| title_full | Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation |
| title_fullStr | Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation |
| title_full_unstemmed | Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation |
| title_short | Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation |
| title_sort | development of piperine loaded solid self nanoemulsifying drug delivery system optimization in vitro ex vivo and in vivo evaluation |
| topic | oral delivery piperine solid self nanoemusifying antimicrobial activity antihypertensive activity |
| url | https://www.mdpi.com/2079-4991/11/11/2920 |
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