Biochemical, Ameliorative and Cytotoxic Effects of Newly Synthesized Curcumin Microemulsions: Evidence from In Vitro and In Vivo Studies

Curcumin is known to exhibit antioxidant and tissue-healing properties and has recently attracted the attention of the biomedical community for potential use in advanced therapies. This work reports the formulation and characterization of oil-in-water F127 microemulsions to enhance the bioavailabili...

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Main Authors: Abbas Rahdar, Mohammad Reza Hajinezhad, Saman Sargazi, Maryam Zaboli, Mahmood Barani, Francesco Baino, Muhammad Bilal, Esmael Sanchooli
Format: Article
Language:English
Published: MDPI AG 2021-03-01
Series:Nanomaterials
Subjects:
Online Access:https://www.mdpi.com/2079-4991/11/3/817
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author Abbas Rahdar
Mohammad Reza Hajinezhad
Saman Sargazi
Maryam Zaboli
Mahmood Barani
Francesco Baino
Muhammad Bilal
Esmael Sanchooli
author_facet Abbas Rahdar
Mohammad Reza Hajinezhad
Saman Sargazi
Maryam Zaboli
Mahmood Barani
Francesco Baino
Muhammad Bilal
Esmael Sanchooli
author_sort Abbas Rahdar
collection DOAJ
description Curcumin is known to exhibit antioxidant and tissue-healing properties and has recently attracted the attention of the biomedical community for potential use in advanced therapies. This work reports the formulation and characterization of oil-in-water F127 microemulsions to enhance the bioavailability of curcumin Microemulsions showed a high encapsulation efficiency and prolonged release. To investigate the interactions of curcumin with one unit of the polymeric chain of surfactant F127, ethyl butyrate, and sodium octanoate, as well as the interaction between ethyl butyrate and one unit of the F127 polymer chain, the Density Functional Theory (DFT) calculations at the M06-2X level of theory, were performed in water solution. The MTT assay was used to assess the cytotoxicity of free and encapsulated curcumin on non-malignant and malignant cell lines. Combination effects were calculated according to Chou-Talalay’s principles. Results of in vitro studies indicated that MCF7 and HepG2 cells were more sensitive to curcumin microemulsions. Moreover, a synergistic relationship was observed between curcumin microemulsions and cisplatin in all affected fractions of MCF7 and HepG2 cells (CI < 0.9). For in vivo investigation, thioacetamide-intoxicated rats received thioacetamide (100 mg/kg Sc) followed by curcumin microemulsions (30 mg/kg Ip). Thioacetamide-intoxicated rats showed elevated serum liver enzymes, blood urea nitrogen (BUN), and creatinine levels, and a significant reduction in liver superoxide dismutase (SOD) and catalase (CAT) activities (<i>p</i> < 0.05). Curcumin microemulsions reduced liver enzymes and serum creatinine and increased the activity of antioxidant enzymes in thioacetamide-treated rats in comparison to the untreated thioacetamide-intoxicated group. Histopathological investigations confirmed the biochemical findings. Overall, the current results showed the desirable hepatoprotective, nephroprotective, and anti-cancer effects of curcumin microemulsions.
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spelling doaj.art-ac6d78e05181487b898480be8ad32c812023-11-21T11:38:04ZengMDPI AGNanomaterials2079-49912021-03-0111381710.3390/nano11030817Biochemical, Ameliorative and Cytotoxic Effects of Newly Synthesized Curcumin Microemulsions: Evidence from In Vitro and In Vivo StudiesAbbas Rahdar0Mohammad Reza Hajinezhad1Saman Sargazi2Maryam Zaboli3Mahmood Barani4Francesco Baino5Muhammad Bilal6Esmael Sanchooli7Department of Physics, University of Zabol, P.O. Box. 98613-35856, Zabol, IranBasic Veterinary Science Department, Veterinary Faculty, University of Zabol, P.O. Box. 98613-35856, Zabol, IranCellular and Molecular Research Center, Resistant Tuberculosis Institute, Zahedan University of Medical Sciences, Zahedan 98167-43463, IranDepartment of Chemistry, University of Birjand, Birjand 97174-34765, IranDepartment of Chemistry, Shahid Bahonar University of Kerman, Kerman 76169-14111, IranInstitute of Materials Physics and Engineering, Applied Science and Technology Department, Politecnico di Torino, Corso Duca degli Abruzzi 24, 10129 Torino, ItalySchool of Life Science and Food Engineering, Huaiyin Institute of Technology, Huaian 223003, ChinaDepartment of Chemistry, University of Zabol, P.O. Box. 98613-35856, Zabol, PIranCurcumin is known to exhibit antioxidant and tissue-healing properties and has recently attracted the attention of the biomedical community for potential use in advanced therapies. This work reports the formulation and characterization of oil-in-water F127 microemulsions to enhance the bioavailability of curcumin Microemulsions showed a high encapsulation efficiency and prolonged release. To investigate the interactions of curcumin with one unit of the polymeric chain of surfactant F127, ethyl butyrate, and sodium octanoate, as well as the interaction between ethyl butyrate and one unit of the F127 polymer chain, the Density Functional Theory (DFT) calculations at the M06-2X level of theory, were performed in water solution. The MTT assay was used to assess the cytotoxicity of free and encapsulated curcumin on non-malignant and malignant cell lines. Combination effects were calculated according to Chou-Talalay’s principles. Results of in vitro studies indicated that MCF7 and HepG2 cells were more sensitive to curcumin microemulsions. Moreover, a synergistic relationship was observed between curcumin microemulsions and cisplatin in all affected fractions of MCF7 and HepG2 cells (CI < 0.9). For in vivo investigation, thioacetamide-intoxicated rats received thioacetamide (100 mg/kg Sc) followed by curcumin microemulsions (30 mg/kg Ip). Thioacetamide-intoxicated rats showed elevated serum liver enzymes, blood urea nitrogen (BUN), and creatinine levels, and a significant reduction in liver superoxide dismutase (SOD) and catalase (CAT) activities (<i>p</i> < 0.05). Curcumin microemulsions reduced liver enzymes and serum creatinine and increased the activity of antioxidant enzymes in thioacetamide-treated rats in comparison to the untreated thioacetamide-intoxicated group. Histopathological investigations confirmed the biochemical findings. Overall, the current results showed the desirable hepatoprotective, nephroprotective, and anti-cancer effects of curcumin microemulsions.https://www.mdpi.com/2079-4991/11/3/817biomaterialsnanocarrieroil-in-water F127 microemulsionscurcuminhepatoprotectiveantioxidant
spellingShingle Abbas Rahdar
Mohammad Reza Hajinezhad
Saman Sargazi
Maryam Zaboli
Mahmood Barani
Francesco Baino
Muhammad Bilal
Esmael Sanchooli
Biochemical, Ameliorative and Cytotoxic Effects of Newly Synthesized Curcumin Microemulsions: Evidence from In Vitro and In Vivo Studies
Nanomaterials
biomaterials
nanocarrier
oil-in-water F127 microemulsions
curcumin
hepatoprotective
antioxidant
title Biochemical, Ameliorative and Cytotoxic Effects of Newly Synthesized Curcumin Microemulsions: Evidence from In Vitro and In Vivo Studies
title_full Biochemical, Ameliorative and Cytotoxic Effects of Newly Synthesized Curcumin Microemulsions: Evidence from In Vitro and In Vivo Studies
title_fullStr Biochemical, Ameliorative and Cytotoxic Effects of Newly Synthesized Curcumin Microemulsions: Evidence from In Vitro and In Vivo Studies
title_full_unstemmed Biochemical, Ameliorative and Cytotoxic Effects of Newly Synthesized Curcumin Microemulsions: Evidence from In Vitro and In Vivo Studies
title_short Biochemical, Ameliorative and Cytotoxic Effects of Newly Synthesized Curcumin Microemulsions: Evidence from In Vitro and In Vivo Studies
title_sort biochemical ameliorative and cytotoxic effects of newly synthesized curcumin microemulsions evidence from in vitro and in vivo studies
topic biomaterials
nanocarrier
oil-in-water F127 microemulsions
curcumin
hepatoprotective
antioxidant
url https://www.mdpi.com/2079-4991/11/3/817
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