Enhanced Antioxidant and Anti-Inflammatory Effects of Self-Nano and Microemulsifying Drug Delivery Systems Containing Curcumin

Turmeric has been used for decades for its antioxidant and anti-inflammatory effect, which is due to an active ingredient isolated from the plant, called curcumin. However, the extremely poor water-solubility of curcumin often limits the bioavailability of the drug. The aim of our experimental work...

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Main Authors: Liza Józsa, Gábor Vasvári, Dávid Sinka, Dániel Nemes, Zoltan Ujhelyi, Miklós Vecsernyés, Judit Váradi, Ferenc Fenyvesi, István Lekli, Alexandra Gyöngyösi, Ildikó Bácskay, Pálma Fehér
Format: Article
Language:English
Published: MDPI AG 2022-10-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/27/19/6652
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author Liza Józsa
Gábor Vasvári
Dávid Sinka
Dániel Nemes
Zoltan Ujhelyi
Miklós Vecsernyés
Judit Váradi
Ferenc Fenyvesi
István Lekli
Alexandra Gyöngyösi
Ildikó Bácskay
Pálma Fehér
author_facet Liza Józsa
Gábor Vasvári
Dávid Sinka
Dániel Nemes
Zoltan Ujhelyi
Miklós Vecsernyés
Judit Váradi
Ferenc Fenyvesi
István Lekli
Alexandra Gyöngyösi
Ildikó Bácskay
Pálma Fehér
author_sort Liza Józsa
collection DOAJ
description Turmeric has been used for decades for its antioxidant and anti-inflammatory effect, which is due to an active ingredient isolated from the plant, called curcumin. However, the extremely poor water-solubility of curcumin often limits the bioavailability of the drug. The aim of our experimental work was to improve the solubility and thus bioavailability of curcumin by developing self-nano/microemulsifying drug delivery systems (SN/MEDDS). Labrasol and Cremophor RH 40 as nonionic surfactants, Transcutol P as co-surfactant and isopropyl myristate as the oily phase were used during the formulation. The average droplet size of SN/MEDDS containing curcumin was between 32 and 405 nm. It was found that the higher oil content resulted in larger particle size. The drug loading efficiency was between 93.11% and 99.12% and all formulations were thermodynamically stable. The curcumin release was studied at pH 6.8, and the release efficiency ranged between 57.3% and 80.9% after 180 min. The results of the MTT cytotoxicity assay on human keratinocyte cells (HaCaT) and colorectal adenocarcinoma cells (Caco-2) showed that the curcumin-containing preparations were non-cytotoxic at 5 <i>w</i>/<i>v</i>%. According to the results of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide dismutase (SOD) assays, SNEDDS showed significantly higher antioxidant activity. The anti-inflammatory effect of the SN/MEDDS was screened by enzyme-linked immunosorbent assay (ELISA). SNEDDS formulated with Labrasol as surfactant, reduced tumor necrosis factor-alpha (TNF-α) and interleukin-1 beta (IL-1β) levels below 60% at a concentration of 10 <i>w</i>/<i>w</i>%. Our results verified the promising use of SN/MEDDS for the delivery of curcumin. This study demonstrates that the SN/MEDDS could be promising alternatives for the formulation of poorly soluble lipophilic compounds with low bioavailability.
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spelling doaj.art-b72424894ac141648bb54fcb6c8a2fe82023-11-23T21:14:57ZengMDPI AGMolecules1420-30492022-10-012719665210.3390/molecules27196652Enhanced Antioxidant and Anti-Inflammatory Effects of Self-Nano and Microemulsifying Drug Delivery Systems Containing CurcuminLiza Józsa0Gábor Vasvári1Dávid Sinka2Dániel Nemes3Zoltan Ujhelyi4Miklós Vecsernyés5Judit Váradi6Ferenc Fenyvesi7István Lekli8Alexandra Gyöngyösi9Ildikó Bácskay10Pálma Fehér11Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryDoctoral School of Pharmaceutical Sciences, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryDoctoral School of Pharmaceutical Sciences, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, H-4032 Debrecen, HungaryTurmeric has been used for decades for its antioxidant and anti-inflammatory effect, which is due to an active ingredient isolated from the plant, called curcumin. However, the extremely poor water-solubility of curcumin often limits the bioavailability of the drug. The aim of our experimental work was to improve the solubility and thus bioavailability of curcumin by developing self-nano/microemulsifying drug delivery systems (SN/MEDDS). Labrasol and Cremophor RH 40 as nonionic surfactants, Transcutol P as co-surfactant and isopropyl myristate as the oily phase were used during the formulation. The average droplet size of SN/MEDDS containing curcumin was between 32 and 405 nm. It was found that the higher oil content resulted in larger particle size. The drug loading efficiency was between 93.11% and 99.12% and all formulations were thermodynamically stable. The curcumin release was studied at pH 6.8, and the release efficiency ranged between 57.3% and 80.9% after 180 min. The results of the MTT cytotoxicity assay on human keratinocyte cells (HaCaT) and colorectal adenocarcinoma cells (Caco-2) showed that the curcumin-containing preparations were non-cytotoxic at 5 <i>w</i>/<i>v</i>%. According to the results of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide dismutase (SOD) assays, SNEDDS showed significantly higher antioxidant activity. The anti-inflammatory effect of the SN/MEDDS was screened by enzyme-linked immunosorbent assay (ELISA). SNEDDS formulated with Labrasol as surfactant, reduced tumor necrosis factor-alpha (TNF-α) and interleukin-1 beta (IL-1β) levels below 60% at a concentration of 10 <i>w</i>/<i>w</i>%. Our results verified the promising use of SN/MEDDS for the delivery of curcumin. This study demonstrates that the SN/MEDDS could be promising alternatives for the formulation of poorly soluble lipophilic compounds with low bioavailability.https://www.mdpi.com/1420-3049/27/19/6652curcuminself-emulsifying systemsdrug deliveryanti-inflammatory effectantioxidant effect
spellingShingle Liza Józsa
Gábor Vasvári
Dávid Sinka
Dániel Nemes
Zoltan Ujhelyi
Miklós Vecsernyés
Judit Váradi
Ferenc Fenyvesi
István Lekli
Alexandra Gyöngyösi
Ildikó Bácskay
Pálma Fehér
Enhanced Antioxidant and Anti-Inflammatory Effects of Self-Nano and Microemulsifying Drug Delivery Systems Containing Curcumin
Molecules
curcumin
self-emulsifying systems
drug delivery
anti-inflammatory effect
antioxidant effect
title Enhanced Antioxidant and Anti-Inflammatory Effects of Self-Nano and Microemulsifying Drug Delivery Systems Containing Curcumin
title_full Enhanced Antioxidant and Anti-Inflammatory Effects of Self-Nano and Microemulsifying Drug Delivery Systems Containing Curcumin
title_fullStr Enhanced Antioxidant and Anti-Inflammatory Effects of Self-Nano and Microemulsifying Drug Delivery Systems Containing Curcumin
title_full_unstemmed Enhanced Antioxidant and Anti-Inflammatory Effects of Self-Nano and Microemulsifying Drug Delivery Systems Containing Curcumin
title_short Enhanced Antioxidant and Anti-Inflammatory Effects of Self-Nano and Microemulsifying Drug Delivery Systems Containing Curcumin
title_sort enhanced antioxidant and anti inflammatory effects of self nano and microemulsifying drug delivery systems containing curcumin
topic curcumin
self-emulsifying systems
drug delivery
anti-inflammatory effect
antioxidant effect
url https://www.mdpi.com/1420-3049/27/19/6652
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