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ι-Carrageenan nanocomposites for enhanced stability and oral bioavailability of curcumin

BACKGROUND: Carrageenan (CRN), a polygalactan consisting of 15 to 40% ester sulfate, is used in oral controlled-release technology due to its viscosity and large molecular weight. Curcumin (Cur) is a highly potent antioxidant and anti-inflammatory agent against various diseases, such as tumors, live...

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Autores principales: Lee, Joo Young, Lee, Sanghee, Choi, Jang Ho, Na, Kun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8502325/
https://www.ncbi.nlm.nih.gov/pubmed/34627398
http://dx.doi.org/10.1186/s40824-021-00236-4
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author Lee, Joo Young
Lee, Sanghee
Choi, Jang Ho
Na, Kun
author_facet Lee, Joo Young
Lee, Sanghee
Choi, Jang Ho
Na, Kun
author_sort Lee, Joo Young
collection PubMed
description BACKGROUND: Carrageenan (CRN), a polygalactan consisting of 15 to 40% ester sulfate, is used in oral controlled-release technology due to its viscosity and large molecular weight. Curcumin (Cur) is a highly potent antioxidant and anti-inflammatory agent against various diseases, such as tumors, liver disease, rheumatism, and Alzheimer’s disease. Although Cur shows excellent effects in the body, it has major problems, such as poor solubility and low bioavailability in water. METHOD: Nanocomposites containing Cur were developed by emulsion technique. Cur@CRN was characterized through the viscosity measurement, size analysis, stability test, and loading efficiency. Antioxidant effects was analyzed with DPPH reagent, and anti-inflammatory effects was analyzed by NFkB/IkBr signaling pathway with wester blot. Cellular interaction was confirmed by flow cytometry and confocal images. Especially, permeability test was demonstrated in MDCK and Caco-2 monolayer cells. RESULTS: Cur@CRN enhanced stability, antioxidant, and anti-inflammatory effects in vitro, compared with other polymer nanocomposites. Sulfate groups (SO(4)(2−)) in CRN are transported across cell membranes by anion exchangers of the SLC26 gene families. We confirmed Caco-2 cells expressed SLC26A2 receptors interacted with CRN, expect for Tween 80 and hydroxypropyl cellulose. In contrary, other cells did not interact with CRN due to non-expression of SLC26A2 receptors. Based on this, Cur@CRN showed 44-fold better permeability than free Cur in MDCK cell assay. CONCLUSION: Enhanced intestinal permeability of Cur can be applied in various health care facilities with significant antioxidant and anti-inflammatory effects compared with nonformulated Cur. Since the CRN composed of nanocomposites has a high molecular weight, high viscosity, and sulfate groups, it will be a platform that can increase the bioavailability of various insoluble drugs as well as Cur. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1186/s40824-021-00236-4.
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spelling pubmed-85023252021-10-20 ι-Carrageenan nanocomposites for enhanced stability and oral bioavailability of curcumin Lee, Joo Young Lee, Sanghee Choi, Jang Ho Na, Kun Biomater Res Research Article BACKGROUND: Carrageenan (CRN), a polygalactan consisting of 15 to 40% ester sulfate, is used in oral controlled-release technology due to its viscosity and large molecular weight. Curcumin (Cur) is a highly potent antioxidant and anti-inflammatory agent against various diseases, such as tumors, liver disease, rheumatism, and Alzheimer’s disease. Although Cur shows excellent effects in the body, it has major problems, such as poor solubility and low bioavailability in water. METHOD: Nanocomposites containing Cur were developed by emulsion technique. Cur@CRN was characterized through the viscosity measurement, size analysis, stability test, and loading efficiency. Antioxidant effects was analyzed with DPPH reagent, and anti-inflammatory effects was analyzed by NFkB/IkBr signaling pathway with wester blot. Cellular interaction was confirmed by flow cytometry and confocal images. Especially, permeability test was demonstrated in MDCK and Caco-2 monolayer cells. RESULTS: Cur@CRN enhanced stability, antioxidant, and anti-inflammatory effects in vitro, compared with other polymer nanocomposites. Sulfate groups (SO(4)(2−)) in CRN are transported across cell membranes by anion exchangers of the SLC26 gene families. We confirmed Caco-2 cells expressed SLC26A2 receptors interacted with CRN, expect for Tween 80 and hydroxypropyl cellulose. In contrary, other cells did not interact with CRN due to non-expression of SLC26A2 receptors. Based on this, Cur@CRN showed 44-fold better permeability than free Cur in MDCK cell assay. CONCLUSION: Enhanced intestinal permeability of Cur can be applied in various health care facilities with significant antioxidant and anti-inflammatory effects compared with nonformulated Cur. Since the CRN composed of nanocomposites has a high molecular weight, high viscosity, and sulfate groups, it will be a platform that can increase the bioavailability of various insoluble drugs as well as Cur. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1186/s40824-021-00236-4. BioMed Central 2021-10-09 /pmc/articles/PMC8502325/ /pubmed/34627398 http://dx.doi.org/10.1186/s40824-021-00236-4 Text en © The Author(s) 2021 https://creativecommons.org/licenses/by/4.0/Open AccessThis article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) . The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/ (https://creativecommons.org/publicdomain/zero/1.0/) ) applies to the data made available in this article, unless otherwise stated in a credit line to the data.
spellingShingle Research Article
Lee, Joo Young
Lee, Sanghee
Choi, Jang Ho
Na, Kun
ι-Carrageenan nanocomposites for enhanced stability and oral bioavailability of curcumin
title ι-Carrageenan nanocomposites for enhanced stability and oral bioavailability of curcumin
title_full ι-Carrageenan nanocomposites for enhanced stability and oral bioavailability of curcumin
title_fullStr ι-Carrageenan nanocomposites for enhanced stability and oral bioavailability of curcumin
title_full_unstemmed ι-Carrageenan nanocomposites for enhanced stability and oral bioavailability of curcumin
title_short ι-Carrageenan nanocomposites for enhanced stability and oral bioavailability of curcumin
title_sort ι-carrageenan nanocomposites for enhanced stability and oral bioavailability of curcumin
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8502325/
https://www.ncbi.nlm.nih.gov/pubmed/34627398
http://dx.doi.org/10.1186/s40824-021-00236-4
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