Improving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges

Atefe Rezaei,1,2 Jaleh Varshosaz,3 Mehrafarin Fesharaki,4 Armin Farhang,2 Seid Mahdi Jafari51Department of Food Science and Technology, School of Nutrition and Food Science, Isfahan University of Medical Sciences, Isfahan, Iran; 2Food Security Research Center, Isfahan University of Medical Sciences,...

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Autores principales: Rezaei A, Varshosaz J, Fesharaki M, Farhang A, Jafari SM
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Publicado: Dove Medical Press 2019
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spelling oai:doaj.org-article:09123ce440074f3fa46843ce29aceedd2021-12-02T04:18:21ZImproving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges1178-2013https://doaj.org/article/09123ce440074f3fa46843ce29aceedd2019-06-01T00:00:00Zhttps://www.dovepress.com/improving-the-solubility-and-in-vitro-cytotoxicity-anticancer-activity-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Atefe Rezaei,1,2 Jaleh Varshosaz,3 Mehrafarin Fesharaki,4 Armin Farhang,2 Seid Mahdi Jafari51Department of Food Science and Technology, School of Nutrition and Food Science, Isfahan University of Medical Sciences, Isfahan, Iran; 2Food Security Research Center, Isfahan University of Medical Sciences, Isfahan, Iran; 3Department of Pharmaceutics, School of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran; 4Department of Cell Science, Research Center Medical Sciences, School of Medicine, Isfahan University of Medical Sciences, Isfahan, Iran; 5Department of Food Materials and Process Design Engineering, Gorgan University of Agricultural Sciences and Natural Resources, Gorgan, IranPurpose: Ferulic acid (FA) is a poorly water-soluble natural antioxidant with anticancer activity. This poor solubility limits the application of FA in the food and pharmaceutical industry. Cyclodextrin nanosponges (CD-NSs) are a novel group of cross-linked CD derivatives which can be used to enhance the solubility of low-soluble bioactive compounds.Methods: In this study, FA was encapsulated into the NSs in the proportion of 1:4 (FA:NS). Diphenyl carbonate was used as a cross-linker in different proportions with β-CD. Characterization of obtained NSs was performed using scanning electron microscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) analysis.Results: Our results revealed that the solubility of encapsulated FA was increased up to fifteenfold compared with pure FA in the proportion of 1:4 (CD:cross-linker). The results of FTIR, XRD, and DSC confirmed the interaction of FA with NSs. The cytotoxicity of encapsulated FA against MCF7 and 4T1 breast cancer cell lines was investigated using different concentrations of FA in 24, 48, and 72 hrs. The cytotoxicity assay indicated that FA treatment reduced viability and enhanced apoptosis of cancer cells. IC50 value of encapsulated FA (250 ppm) was decreased by threefold when compared with pure FA (750 ppm).Conclusion: In general, CD-NS was found to be a suitable delivery system for poorly soluble bioactives such as FA.Keywords: nanoencapsulation, nanosponges, cyclodextrins, ferulic acid, cytotoxicityRezaei AVarshosaz JFesharaki MFarhang AJafari SMDove Medical PressarticleNanoencapsulationnanospongescyclodextrinsferulic acidcytotoxicity.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 4589-4599 (2019)
institution DOAJ
collection DOAJ
language EN
topic Nanoencapsulation
nanosponges
cyclodextrins
ferulic acid
cytotoxicity.
Medicine (General)
R5-920
spellingShingle Nanoencapsulation
nanosponges
cyclodextrins
ferulic acid
cytotoxicity.
Medicine (General)
R5-920
Rezaei A
Varshosaz J
Fesharaki M
Farhang A
Jafari SM
Improving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges
description Atefe Rezaei,1,2 Jaleh Varshosaz,3 Mehrafarin Fesharaki,4 Armin Farhang,2 Seid Mahdi Jafari51Department of Food Science and Technology, School of Nutrition and Food Science, Isfahan University of Medical Sciences, Isfahan, Iran; 2Food Security Research Center, Isfahan University of Medical Sciences, Isfahan, Iran; 3Department of Pharmaceutics, School of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran; 4Department of Cell Science, Research Center Medical Sciences, School of Medicine, Isfahan University of Medical Sciences, Isfahan, Iran; 5Department of Food Materials and Process Design Engineering, Gorgan University of Agricultural Sciences and Natural Resources, Gorgan, IranPurpose: Ferulic acid (FA) is a poorly water-soluble natural antioxidant with anticancer activity. This poor solubility limits the application of FA in the food and pharmaceutical industry. Cyclodextrin nanosponges (CD-NSs) are a novel group of cross-linked CD derivatives which can be used to enhance the solubility of low-soluble bioactive compounds.Methods: In this study, FA was encapsulated into the NSs in the proportion of 1:4 (FA:NS). Diphenyl carbonate was used as a cross-linker in different proportions with β-CD. Characterization of obtained NSs was performed using scanning electron microscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) analysis.Results: Our results revealed that the solubility of encapsulated FA was increased up to fifteenfold compared with pure FA in the proportion of 1:4 (CD:cross-linker). The results of FTIR, XRD, and DSC confirmed the interaction of FA with NSs. The cytotoxicity of encapsulated FA against MCF7 and 4T1 breast cancer cell lines was investigated using different concentrations of FA in 24, 48, and 72 hrs. The cytotoxicity assay indicated that FA treatment reduced viability and enhanced apoptosis of cancer cells. IC50 value of encapsulated FA (250 ppm) was decreased by threefold when compared with pure FA (750 ppm).Conclusion: In general, CD-NS was found to be a suitable delivery system for poorly soluble bioactives such as FA.Keywords: nanoencapsulation, nanosponges, cyclodextrins, ferulic acid, cytotoxicity
format article
author Rezaei A
Varshosaz J
Fesharaki M
Farhang A
Jafari SM
author_facet Rezaei A
Varshosaz J
Fesharaki M
Farhang A
Jafari SM
author_sort Rezaei A
title Improving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges
title_short Improving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges
title_full Improving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges
title_fullStr Improving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges
title_full_unstemmed Improving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges
title_sort improving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges
publisher Dove Medical Press
publishDate 2019
url https://doaj.org/article/09123ce440074f3fa46843ce29aceedd
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