Curcumin and Quercetin-Loaded Lipid Nanocarriers: Development of Omega-3 Mucoadhesive Nanoemulsions for Intranasal Administration

Curcumin (CUR) and quercetin (QU) are potential compounds for treatment of brain diseases such as neurodegenerative diseases (ND) because of their anti-inflammatory and antioxidant properties. However, low water solubility and poor bioavailability hinder their clinical use. In this context, nanotech...

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Published inNanomaterials (Basel, Switzerland) Vol. 12; no. 7; p. 1073
Main Authors Vaz, Gustavo Richter, Carrasco, Mariana Corrêa Falkembach, Batista, Matheus Monteiro, Barros, Paula Alice Bezerra, Oliveira, Meliza da Conceição, Muccillo-Baisch, Ana Luiza, Yurgel, Virginia Campello, Buttini, Francesca, Soares, Félix Alexandre Antunes, Cordeiro, Larissa Marafiga, Fachel, Flavia, Teixeira, Helder Ferreira, Bidone, Juliana, de Oliveira, Patrícia Diaz, Sonvico, Fabio, Dora, Cristiana Lima
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 25.03.2022
MDPI
Subjects
Antioxidants
Bioavailability
Biocompatibility
Biopharmaceuticals
Brain
Chloride
Controlled release
Curcumin
Ethanol
Fatty acids
Formulations
Health services
Inflammation
Intranasal administration
Lipids
Nanoemulsions
Nanotechnology
Nervous system
Neurodegenerative diseases
Penetration
Pharmaceuticals
Polyethylene glycol
Polyphenols
Quercetin
Surfactants
Sustained release
Toxicity
Viscosity
Zeta potential
Brazil
United States > US
Germany
toxicity
nanoemulsions
quercetin
intranasal administration
curcumin
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Abstract Curcumin (CUR) and quercetin (QU) are potential compounds for treatment of brain diseases such as neurodegenerative diseases (ND) because of their anti-inflammatory and antioxidant properties. However, low water solubility and poor bioavailability hinder their clinical use. In this context, nanotechnology arises as a strategy to overcome biopharmaceutical issues. In this work, we develop, characterize, compare, and optimize three different omega-3 (ω-3) fatty acids nanoemulsions (NEs) loaded with CUR and QU (negative, cationic, gelling) prepared by two different methods for administration by intranasal route (IN). The results showed that formulations prepared with the two proposed methods exhibited good stability and were able to incorporate a similar amount of CUR and QU. On the other side, differences in size, zeta potential, in vitro release kinetics, and permeation/retention test were observed. Considering the two preparation methods tested, high-pressure homogenization (HPH) shows advantages, and the CQ NE- obtained demonstrated potential for sustained release. Toxicity studies demonstrated that the formulations were not toxic for . The developed ω-3 fatty acid NEs have shown a range of interesting properties for the treatment of brain diseases, since they have the potential to increase the nose-to-brain permeation of CUR and QU, enabling enhanced treatments efficiency.
AbstractList Curcumin (CUR) and quercetin (QU) are potential compounds for treatment of brain diseases such as neurodegenerative diseases (ND) because of their anti-inflammatory and antioxidant properties. However, low water solubility and poor bioavailability hinder their clinical use. In this context, nanotechnology arises as a strategy to overcome biopharmaceutical issues. In this work, we develop, characterize, compare, and optimize three different omega-3 (ω-3) fatty acids nanoemulsions (NEs) loaded with CUR and QU (negative, cationic, gelling) prepared by two different methods for administration by intranasal route (IN). The results showed that formulations prepared with the two proposed methods exhibited good stability and were able to incorporate a similar amount of CUR and QU. On the other side, differences in size, zeta potential, in vitro release kinetics, and permeation/retention test were observed. Considering the two preparation methods tested, high-pressure homogenization (HPH) shows advantages, and the CQ NE- obtained demonstrated potential for sustained release. Toxicity studies demonstrated that the formulations were not toxic for Caenorhabditis elegans . The developed ω-3 fatty acid NEs have shown a range of interesting properties for the treatment of brain diseases, since they have the potential to increase the nose-to-brain permeation of CUR and QU, enabling enhanced treatments efficiency.
Curcumin (CUR) and quercetin (QU) are potential compounds for treatment of brain diseases such as neurodegenerative diseases (ND) because of their anti-inflammatory and antioxidant properties. However, low water solubility and poor bioavailability hinder their clinical use. In this context, nanotechnology arises as a strategy to overcome biopharmaceutical issues. In this work, we develop, characterize, compare, and optimize three different omega-3 (ω-3) fatty acids nanoemulsions (NEs) loaded with CUR and QU (negative, cationic, gelling) prepared by two different methods for administration by intranasal route (IN). The results showed that formulations prepared with the two proposed methods exhibited good stability and were able to incorporate a similar amount of CUR and QU. On the other side, differences in size, zeta potential, in vitro release kinetics, and permeation/retention test were observed. Considering the two preparation methods tested, high-pressure homogenization (HPH) shows advantages, and the CQ NE- obtained demonstrated potential for sustained release. Toxicity studies demonstrated that the formulations were not toxic for . The developed ω-3 fatty acid NEs have shown a range of interesting properties for the treatment of brain diseases, since they have the potential to increase the nose-to-brain permeation of CUR and QU, enabling enhanced treatments efficiency.
Curcumin (CUR) and quercetin (QU) are potential compounds for treatment of brain diseases such as neurodegenerative diseases (ND) because of their anti-inflammatory and antioxidant properties. However, low water solubility and poor bioavailability hinder their clinical use. In this context, nanotechnology arises as a strategy to overcome biopharmaceutical issues. In this work, we develop, characterize, compare, and optimize three different omega-3 (ω-3) fatty acids nanoemulsions (NEs) loaded with CUR and QU (negative, cationic, gelling) prepared by two different methods for administration by intranasal route (IN). The results showed that formulations prepared with the two proposed methods exhibited good stability and were able to incorporate a similar amount of CUR and QU. On the other side, differences in size, zeta potential, in vitro release kinetics, and permeation/retention test were observed. Considering the two preparation methods tested, high-pressure homogenization (HPH) shows advantages, and the CQ NE- obtained demonstrated potential for sustained release. Toxicity studies demonstrated that the formulations were not toxic for Caenorhabditis elegans. The developed ω-3 fatty acid NEs have shown a range of interesting properties for the treatment of brain diseases, since they have the potential to increase the nose-to-brain permeation of CUR and QU, enabling enhanced treatments efficiency.
Author Fachel, Flavia
Buttini, Francesca
de Oliveira, Patrícia Diaz
Dora, Cristiana Lima
Sonvico, Fabio
Batista, Matheus Monteiro
Barros, Paula Alice Bezerra
Muccillo-Baisch, Ana Luiza
Bidone, Juliana
Soares, Félix Alexandre Antunes
Carrasco, Mariana Corrêa Falkembach
Oliveira, Meliza da Conceição
Cordeiro, Larissa Marafiga
Teixeira, Helder Ferreira
Vaz, Gustavo Richter
Yurgel, Virginia Campello
AuthorAffiliation 1 Graduate Program in Health Sciences, Federal University of Rio Grande, Rio Grande 96203-900, Brazil; richtervaz@gmail.com (G.R.V.); mari_falkembach@hotmail.com (M.C.F.C.); mbmatheus54@gmail.com (M.M.B.); alicebarros.pb@gmail.com (P.A.B.B.); melizacoliveira@hotmail.com (M.d.C.O.); anabaisch@gmail.com (A.L.M.-B.); virginia.yurgel@gmail.com (V.C.Y.)
2 Food and Drug Department, University of Parma, 43124 Parma, Italy; francesca.buttini@unipr.it (F.B.); fabio.sonvico@unipr.it (F.S.)
3 Graduate Program in Biological Sciences, Federal University of Santa Maria, Santa Maria 97105-900, Brazil; felix@ufsm.br (F.A.A.S.); larissa.marafiga@hotmail.com (L.M.C.)
4 Graduate Program in Pharmaceutical Sciences, Federal University of Rio Grande do Sul, Porto Alegre 90610-000, Brazil; flavia_fachel@hotmail.com (F.F.); helder.teixeira@ufrgs.br (H.F.T.)
5 Center of Chemical, Pharmaceutical and Food Sciences, Federal University of Pelotas, Pelotas 96010-610, Brazil; julianabidone@gmail.com
6 Department of Biote
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BackLink https://www.ncbi.nlm.nih.gov/pubmed/35407191$$D View this record in MEDLINE/PubMed
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Issue 7
Keywords toxicity
nanoemulsions
quercetin
intranasal administration
curcumin
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PublicationCentury 2000
PublicationDate 20220325
PublicationDateYYYYMMDD 2022-03-25
PublicationDate_xml – month: 3
  year: 2022
  text: 20220325
  day: 25
PublicationDecade 2020
PublicationPlace Switzerland
PublicationPlace_xml – name: Switzerland
– name: Basel
PublicationTitle Nanomaterials (Basel, Switzerland)
PublicationTitleAlternate Nanomaterials (Basel)
PublicationYear 2022
Publisher MDPI AG
MDPI
Publisher_xml – name: MDPI AG
– name: MDPI
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Snippet Curcumin (CUR) and quercetin (QU) are potential compounds for treatment of brain diseases such as neurodegenerative diseases (ND) because of their...
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SubjectTerms Antioxidants
Bioavailability
Biocompatibility
Biopharmaceuticals
Brain
Chloride
Controlled release
Curcumin
Ethanol
Fatty acids
Formulations
Health services
Inflammation
Intranasal administration
Lipids
Nanoemulsions
Nanotechnology
Nervous system
Neurodegenerative diseases
Penetration
Pharmaceuticals
Polyethylene glycol
Polyphenols
Quercetin
Surfactants
Sustained release
Toxicity
Viscosity
Zeta potential
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Title Curcumin and Quercetin-Loaded Lipid Nanocarriers: Development of Omega-3 Mucoadhesive Nanoemulsions for Intranasal Administration
URI https://www.ncbi.nlm.nih.gov/pubmed/35407191
https://www.proquest.com/docview/2649067856
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https://pubmed.ncbi.nlm.nih.gov/PMC9000715
https://doaj.org/article/784a8a1696f0490d8197ce88f858aa7a
Volume 12
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