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...

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Autores principales:	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
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	oral delivery piperine solid self nanoemusifying antimicrobial activity antihypertensive activity Chemistry QD1-999
Acceso en línea:	https://doaj.org/article/8140c9b4db6f448683e47472324060ea
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spelling	oai:doaj.org-article:8140c9b4db6f448683e47472324060ea2021-11-25T18:30:52ZDevelopment of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation10.3390/nano111129202079-4991https://doaj.org/article/8140c9b4db6f448683e47472324060ea2021-10-01T00:00:00Zhttps://www.mdpi.com/2079-4991/11/11/2920https://doaj.org/toc/2079-4991Hypertension 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.Ameeduzzafar ZafarSyed Sarim ImamNabil K. AlruwailiOmar Awad AlsaidanMohammed H. ElkomyMohammed M. GhoneimSultan AlshehriAhmed Mahmoud Abdelhaleem AliKhalid Saad AlharbiMohd YasirKaveripakkam M. NoorullaSami I. AlzareaAbdullah S. AlanaziMDPI AGarticleoral deliverypiperinesolid self nanoemusifyingantimicrobial activityantihypertensive activityChemistryQD1-999ENNanomaterials, Vol 11, Iss 2920, p 2920 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	oral delivery piperine solid self nanoemusifying antimicrobial activity antihypertensive activity Chemistry QD1-999
spellingShingle	oral delivery piperine solid self nanoemusifying antimicrobial activity antihypertensive activity Chemistry QD1-999 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
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.
format	article
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
title	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_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_sort	development of piperine-loaded solid self-nanoemulsifying drug delivery system: optimization, in-vitro, ex-vivo, and in-vivo evaluation
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/8140c9b4db6f448683e47472324060ea
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Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

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