A green approach for the sustained-intestinal delivery of red chili (Capsicum annum L) extracted capsaicinoids with enhanced bioavailability

Intestinal delivery with enhanced bioavailability is of great significance for stomach irritating and pungent bioactive molecules. The present study reports the development of a pungency-masked food-grade microbeadlets for the sustained-intestinal delivery of red chili extracted capsaicinoids using...

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Main Authors: Ashil Joseph, Abhilash Maliakkal Balakrishnan, Johannah Natinga Mulakal, Syam Das Sivadasan, Ratheesh Mohan, Balu Maliakel, Krishnakumar Illathu Madhavamenon
Format: Article
Language:English
Published: Elsevier 2021-10-01
Series:Journal of Functional Foods
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S1756464621003078
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author Ashil Joseph
Abhilash Maliakkal Balakrishnan
Johannah Natinga Mulakal
Syam Das Sivadasan
Ratheesh Mohan
Balu Maliakel
Krishnakumar Illathu Madhavamenon
author_facet Ashil Joseph
Abhilash Maliakkal Balakrishnan
Johannah Natinga Mulakal
Syam Das Sivadasan
Ratheesh Mohan
Balu Maliakel
Krishnakumar Illathu Madhavamenon
author_sort Ashil Joseph
collection DOAJ
description Intestinal delivery with enhanced bioavailability is of great significance for stomach irritating and pungent bioactive molecules. The present study reports the development of a pungency-masked food-grade microbeadlets for the sustained-intestinal delivery of red chili extracted capsaicinoids using fenugreek galactomannans. Capsaicinoids encapsulated microbeads (CapF) of about 250 to 400 µm were prepared by a gel-phase homogenization, fluid-bed granulation followed by galactomannan coating, and characterized by NMR, FTIR, DSC, PXRD, and SEM as stable, directly compressible, free flowing amorphous beadlets with a tap density of 0.64 ± 0.2 g/mL. Swelling studies, in vitro release kinetics and particle size analysis indicated the intestinal delivery of soluble capsaicinoids. Pharmacokinetic studies on Wistar rats revealed enhanced bioavailability (19-fold) of CapF when the area under plasma concentration verses time was compared with that of unformulated capsaicinoids. CapF was safe upon gastric mucosa irritation test and demonstrated significant (P < 0.05) anti-obesity effect in high fat diet-induced hypercholesteremic rats.
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spelling doaj.art-7fe8241e31284e5ea12d6fd60027e9242022-12-21T18:28:37ZengElsevierJournal of Functional Foods1756-46462021-10-0185104658A green approach for the sustained-intestinal delivery of red chili (Capsicum annum L) extracted capsaicinoids with enhanced bioavailabilityAshil Joseph0Abhilash Maliakkal Balakrishnan1Johannah Natinga Mulakal2Syam Das Sivadasan3Ratheesh Mohan4Balu Maliakel5Krishnakumar Illathu Madhavamenon6R&D Center, Akay Natural Ingredients, Ambunadu, Cochin 683561, IndiaR&D Center, Akay Natural Ingredients, Ambunadu, Cochin 683561, IndiaR&D Center, Akay Natural Ingredients, Ambunadu, Cochin 683561, IndiaR&D Center, Akay Natural Ingredients, Ambunadu, Cochin 683561, IndiaDepartment of Biochemistry, St. Thomas College, Pala, Kerala, IndiaR&D Center, Akay Natural Ingredients, Ambunadu, Cochin 683561, IndiaR&D Center, Akay Natural Ingredients, Ambunadu, Cochin 683561, India; Corresponding author at: R&D Center, Akay Natural Ingredients, Ambunadu, Malaidamthuruth P. O., Cochin 683561, India.Intestinal delivery with enhanced bioavailability is of great significance for stomach irritating and pungent bioactive molecules. The present study reports the development of a pungency-masked food-grade microbeadlets for the sustained-intestinal delivery of red chili extracted capsaicinoids using fenugreek galactomannans. Capsaicinoids encapsulated microbeads (CapF) of about 250 to 400 µm were prepared by a gel-phase homogenization, fluid-bed granulation followed by galactomannan coating, and characterized by NMR, FTIR, DSC, PXRD, and SEM as stable, directly compressible, free flowing amorphous beadlets with a tap density of 0.64 ± 0.2 g/mL. Swelling studies, in vitro release kinetics and particle size analysis indicated the intestinal delivery of soluble capsaicinoids. Pharmacokinetic studies on Wistar rats revealed enhanced bioavailability (19-fold) of CapF when the area under plasma concentration verses time was compared with that of unformulated capsaicinoids. CapF was safe upon gastric mucosa irritation test and demonstrated significant (P < 0.05) anti-obesity effect in high fat diet-induced hypercholesteremic rats.http://www.sciencedirect.com/science/article/pii/S1756464621003078BeadletsCapsicum annum LCapsaicinCapsifenFenugreek dietary fiberHydrogel
spellingShingle Ashil Joseph
Abhilash Maliakkal Balakrishnan
Johannah Natinga Mulakal
Syam Das Sivadasan
Ratheesh Mohan
Balu Maliakel
Krishnakumar Illathu Madhavamenon
A green approach for the sustained-intestinal delivery of red chili (Capsicum annum L) extracted capsaicinoids with enhanced bioavailability
Journal of Functional Foods
Beadlets
Capsicum annum L
Capsaicin
Capsifen
Fenugreek dietary fiber
Hydrogel
title A green approach for the sustained-intestinal delivery of red chili (Capsicum annum L) extracted capsaicinoids with enhanced bioavailability
title_full A green approach for the sustained-intestinal delivery of red chili (Capsicum annum L) extracted capsaicinoids with enhanced bioavailability
title_fullStr A green approach for the sustained-intestinal delivery of red chili (Capsicum annum L) extracted capsaicinoids with enhanced bioavailability
title_full_unstemmed A green approach for the sustained-intestinal delivery of red chili (Capsicum annum L) extracted capsaicinoids with enhanced bioavailability
title_short A green approach for the sustained-intestinal delivery of red chili (Capsicum annum L) extracted capsaicinoids with enhanced bioavailability
title_sort green approach for the sustained intestinal delivery of red chili capsicum annum l extracted capsaicinoids with enhanced bioavailability
topic Beadlets
Capsicum annum L
Capsaicin
Capsifen
Fenugreek dietary fiber
Hydrogel
url http://www.sciencedirect.com/science/article/pii/S1756464621003078
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