Cargando…

Fiber-Reinforced-Phospholipid Vehicle-Based Delivery of l-Ascorbic Acid: Development, Characterization, ADMET Profiling, and Efficacy by a Randomized, Single-Dose, Crossover Oral Bioavailability Study

[Image: see text] l-ascorbic acid (AA) or vitamin C is a crucial nutrient needed for optimal health. However, being unable to be synthesized by the body, it is thus necessary to be included in health care products. Moreover, AA is one of the antioxidants that occur naturally, which is used in pharma...

Descripción completa

Detalles Bibliográficos
Autores principales: Jacob, Joby, Sukumaran, Nimisha Pulikkal, Jude, Shintu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7931380/
https://www.ncbi.nlm.nih.gov/pubmed/33681596
http://dx.doi.org/10.1021/acsomega.0c05963
_version_ 1783660280413159424
author Jacob, Joby
Sukumaran, Nimisha Pulikkal
Jude, Shintu
author_facet Jacob, Joby
Sukumaran, Nimisha Pulikkal
Jude, Shintu
author_sort Jacob, Joby
collection PubMed
description [Image: see text] l-ascorbic acid (AA) or vitamin C is a crucial nutrient needed for optimal health. However, being unable to be synthesized by the body, it is thus necessary to be included in health care products. Moreover, AA is one of the antioxidants that occur naturally, which is used in pharmaceutical and food products as an antioxidant additive. However, AA is vulnerable to environmental settings and undergoes oxidative degradation to dehydroascorbic acid and further to inactive products. Therefore, new research strategies and approaches are required to augment its stability. The objective of this study is to develop and characterize a fiber-reinforced-phospholipid (FRP) matrix-based vehicle, Zeal-AA, for the delivery of AA and optimize the oral bioavailability of the obtained AA powder using an efficacy study by open-label, randomized, single-dose, two-treatment, two-sequence, two-period, two-way crossover. The structural and surface morphologies were analyzed by Fourier transform infrared spectroscopy, transmission electron microscopy, scanning electron microscopy, and differential scanning calorimetry studies. Encapsulation efficiency, mean particle size, size distribution, ζ-potential measurements, and ADMET profiling revealed the potential delivery system for AA. AUC(0–t) was found to be 55.23 (mg/dL) for Zeal-AA, whereas it was 9.38 (mg/dL) for AA, and C(max) was found to be 6.69 (mg/dL) for Zeal-AA, whereas it was 1.23 (mg/dL) for AA, with a fold difference of bioavailability in terms of AUC found to be 5.9 fold. The results show that a single oral dose of Zeal-AA is capable of rising the AA levels in the body relative to the control up to 24 h.
format Online
Article
Text
id pubmed-7931380
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher American Chemical Society
record_format MEDLINE/PubMed
spelling pubmed-79313802021-03-05 Fiber-Reinforced-Phospholipid Vehicle-Based Delivery of l-Ascorbic Acid: Development, Characterization, ADMET Profiling, and Efficacy by a Randomized, Single-Dose, Crossover Oral Bioavailability Study Jacob, Joby Sukumaran, Nimisha Pulikkal Jude, Shintu ACS Omega [Image: see text] l-ascorbic acid (AA) or vitamin C is a crucial nutrient needed for optimal health. However, being unable to be synthesized by the body, it is thus necessary to be included in health care products. Moreover, AA is one of the antioxidants that occur naturally, which is used in pharmaceutical and food products as an antioxidant additive. However, AA is vulnerable to environmental settings and undergoes oxidative degradation to dehydroascorbic acid and further to inactive products. Therefore, new research strategies and approaches are required to augment its stability. The objective of this study is to develop and characterize a fiber-reinforced-phospholipid (FRP) matrix-based vehicle, Zeal-AA, for the delivery of AA and optimize the oral bioavailability of the obtained AA powder using an efficacy study by open-label, randomized, single-dose, two-treatment, two-sequence, two-period, two-way crossover. The structural and surface morphologies were analyzed by Fourier transform infrared spectroscopy, transmission electron microscopy, scanning electron microscopy, and differential scanning calorimetry studies. Encapsulation efficiency, mean particle size, size distribution, ζ-potential measurements, and ADMET profiling revealed the potential delivery system for AA. AUC(0–t) was found to be 55.23 (mg/dL) for Zeal-AA, whereas it was 9.38 (mg/dL) for AA, and C(max) was found to be 6.69 (mg/dL) for Zeal-AA, whereas it was 1.23 (mg/dL) for AA, with a fold difference of bioavailability in terms of AUC found to be 5.9 fold. The results show that a single oral dose of Zeal-AA is capable of rising the AA levels in the body relative to the control up to 24 h. American Chemical Society 2021-02-17 /pmc/articles/PMC7931380/ /pubmed/33681596 http://dx.doi.org/10.1021/acsomega.0c05963 Text en © 2021 The Authors. Published by American Chemical Society This is an open access article published under an ACS AuthorChoice License (https://creativecommons.org/licenses/by-nc-nd/4.0/) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
spellingShingle Jacob, Joby
Sukumaran, Nimisha Pulikkal
Jude, Shintu
Fiber-Reinforced-Phospholipid Vehicle-Based Delivery of l-Ascorbic Acid: Development, Characterization, ADMET Profiling, and Efficacy by a Randomized, Single-Dose, Crossover Oral Bioavailability Study
title Fiber-Reinforced-Phospholipid Vehicle-Based Delivery of l-Ascorbic Acid: Development, Characterization, ADMET Profiling, and Efficacy by a Randomized, Single-Dose, Crossover Oral Bioavailability Study
title_full Fiber-Reinforced-Phospholipid Vehicle-Based Delivery of l-Ascorbic Acid: Development, Characterization, ADMET Profiling, and Efficacy by a Randomized, Single-Dose, Crossover Oral Bioavailability Study
title_fullStr Fiber-Reinforced-Phospholipid Vehicle-Based Delivery of l-Ascorbic Acid: Development, Characterization, ADMET Profiling, and Efficacy by a Randomized, Single-Dose, Crossover Oral Bioavailability Study
title_full_unstemmed Fiber-Reinforced-Phospholipid Vehicle-Based Delivery of l-Ascorbic Acid: Development, Characterization, ADMET Profiling, and Efficacy by a Randomized, Single-Dose, Crossover Oral Bioavailability Study
title_short Fiber-Reinforced-Phospholipid Vehicle-Based Delivery of l-Ascorbic Acid: Development, Characterization, ADMET Profiling, and Efficacy by a Randomized, Single-Dose, Crossover Oral Bioavailability Study
title_sort fiber-reinforced-phospholipid vehicle-based delivery of l-ascorbic acid: development, characterization, admet profiling, and efficacy by a randomized, single-dose, crossover oral bioavailability study
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7931380/
https://www.ncbi.nlm.nih.gov/pubmed/33681596
http://dx.doi.org/10.1021/acsomega.0c05963
work_keys_str_mv AT jacobjoby fiberreinforcedphospholipidvehiclebaseddeliveryoflascorbicaciddevelopmentcharacterizationadmetprofilingandefficacybyarandomizedsingledosecrossoveroralbioavailabilitystudy
AT sukumarannimishapulikkal fiberreinforcedphospholipidvehiclebaseddeliveryoflascorbicaciddevelopmentcharacterizationadmetprofilingandefficacybyarandomizedsingledosecrossoveroralbioavailabilitystudy
AT judeshintu fiberreinforcedphospholipidvehiclebaseddeliveryoflascorbicaciddevelopmentcharacterizationadmetprofilingandefficacybyarandomizedsingledosecrossoveroralbioavailabilitystudy