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Physico-Chemical Characterization and Biopharmaceutical Evaluation of Lipid-Poloxamer-Based Organogels for Curcumin Skin Delivery

Organogels (ORGs) are semi-solid materials, in which an organic phase is immobilized by a three-dimensional network composed of self-organized system, forming the aqueous phase. In this context, lipid–Pluronics (PLs) ORGs form a two-phase system which can be effectively used as skin delivery systems...

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Autores principales: Vigato, Aryane Alves, Querobino, Samyr Machado, de Faria, Naially Cardoso, Candido, Ana Carolina Bolela Bovo, Magalhães, Lizandra Guidi, Cereda, Cíntia Maria Saia, Tófoli, Giovana Radomille, Campos, Estefânia Vangelie Ramos, Machado, Ian Pompermayer, Fraceto, Leonardo Fernandes, de Sairre, Mirela Inês, de Araujo, Daniele Ribeiro
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6751402/
https://www.ncbi.nlm.nih.gov/pubmed/31572185
http://dx.doi.org/10.3389/fphar.2019.01006
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author Vigato, Aryane Alves
Querobino, Samyr Machado
de Faria, Naially Cardoso
Candido, Ana Carolina Bolela Bovo
Magalhães, Lizandra Guidi
Cereda, Cíntia Maria Saia
Tófoli, Giovana Radomille
Campos, Estefânia Vangelie Ramos
Machado, Ian Pompermayer
Fraceto, Leonardo Fernandes
de Sairre, Mirela Inês
de Araujo, Daniele Ribeiro
author_facet Vigato, Aryane Alves
Querobino, Samyr Machado
de Faria, Naially Cardoso
Candido, Ana Carolina Bolela Bovo
Magalhães, Lizandra Guidi
Cereda, Cíntia Maria Saia
Tófoli, Giovana Radomille
Campos, Estefânia Vangelie Ramos
Machado, Ian Pompermayer
Fraceto, Leonardo Fernandes
de Sairre, Mirela Inês
de Araujo, Daniele Ribeiro
author_sort Vigato, Aryane Alves
collection PubMed
description Organogels (ORGs) are semi-solid materials, in which an organic phase is immobilized by a three-dimensional network composed of self-organized system, forming the aqueous phase. In this context, lipid–Pluronics (PLs) ORGs form a two-phase system which can be effectively used as skin delivery systems, favoring their permeation across the skin. In this study, we presented the development of ORG skin drug-delivery systems for curcumin (CUR), a liposoluble phenolic pigment extracted from the turmeric rhizome. In special, we designed the formulation compositions in order to carry high amounts of CUR soluble in oleic acid (OA), as organic phase, entrapped into an aqueous phase composed of micellar PL-based hydrogels by associating two polymers with different hydrophilic–lipophilic balances, Pluronic F-127 (PL F-127), and Pluronic L-81 (PL L-81), to enhance the permeation across the skin. Results revealed that the incorporation of PL L-81 favored the CUR incorporation into micelle–micelle interface. CUR insertion into OA-PL F-127/L-81 reduced both G’/G” relationship (∼16 x) and viscosity values (η* ∼ 54 mPa.s, at 32.5°C), disturbing the ORG network structural organization. In vitro permeation assays through Strat-M(®) skin-model membranes showed that higher CUR-permeated amounts were obtained for OA-PL F-127/L-81 (4.83 µg.cm(−2)) compared to OA-PL F-127 (3.51 μg.cm(−2)) and OA (2.25 μg.cm(−2)) or hydrogels (∼1.2 μg.cm(−2), p < 0.001). Additionally, ORG formulations presented low cytotoxic effects and evoked pronounced antileishmanial activity (IC(50) < 1.25 µg.ml(−1)), suggesting their potential use as skin delivery systems against Leishmania amazonensis. Results from this study pointed out OA-PL-based ORGs as promising new formulations for possible CUR topical administration.
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spelling pubmed-67514022019-09-30 Physico-Chemical Characterization and Biopharmaceutical Evaluation of Lipid-Poloxamer-Based Organogels for Curcumin Skin Delivery Vigato, Aryane Alves Querobino, Samyr Machado de Faria, Naially Cardoso Candido, Ana Carolina Bolela Bovo Magalhães, Lizandra Guidi Cereda, Cíntia Maria Saia Tófoli, Giovana Radomille Campos, Estefânia Vangelie Ramos Machado, Ian Pompermayer Fraceto, Leonardo Fernandes de Sairre, Mirela Inês de Araujo, Daniele Ribeiro Front Pharmacol Pharmacology Organogels (ORGs) are semi-solid materials, in which an organic phase is immobilized by a three-dimensional network composed of self-organized system, forming the aqueous phase. In this context, lipid–Pluronics (PLs) ORGs form a two-phase system which can be effectively used as skin delivery systems, favoring their permeation across the skin. In this study, we presented the development of ORG skin drug-delivery systems for curcumin (CUR), a liposoluble phenolic pigment extracted from the turmeric rhizome. In special, we designed the formulation compositions in order to carry high amounts of CUR soluble in oleic acid (OA), as organic phase, entrapped into an aqueous phase composed of micellar PL-based hydrogels by associating two polymers with different hydrophilic–lipophilic balances, Pluronic F-127 (PL F-127), and Pluronic L-81 (PL L-81), to enhance the permeation across the skin. Results revealed that the incorporation of PL L-81 favored the CUR incorporation into micelle–micelle interface. CUR insertion into OA-PL F-127/L-81 reduced both G’/G” relationship (∼16 x) and viscosity values (η* ∼ 54 mPa.s, at 32.5°C), disturbing the ORG network structural organization. In vitro permeation assays through Strat-M(®) skin-model membranes showed that higher CUR-permeated amounts were obtained for OA-PL F-127/L-81 (4.83 µg.cm(−2)) compared to OA-PL F-127 (3.51 μg.cm(−2)) and OA (2.25 μg.cm(−2)) or hydrogels (∼1.2 μg.cm(−2), p < 0.001). Additionally, ORG formulations presented low cytotoxic effects and evoked pronounced antileishmanial activity (IC(50) < 1.25 µg.ml(−1)), suggesting their potential use as skin delivery systems against Leishmania amazonensis. Results from this study pointed out OA-PL-based ORGs as promising new formulations for possible CUR topical administration. Frontiers Media S.A. 2019-09-12 /pmc/articles/PMC6751402/ /pubmed/31572185 http://dx.doi.org/10.3389/fphar.2019.01006 Text en Copyright © 2019 Vigato, Querobino, de Faria, Candido, Magalhães, Cereda, Tófoli, Campos, Machado, Fraceto, de Sairre and de Araujo http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Pharmacology
Vigato, Aryane Alves
Querobino, Samyr Machado
de Faria, Naially Cardoso
Candido, Ana Carolina Bolela Bovo
Magalhães, Lizandra Guidi
Cereda, Cíntia Maria Saia
Tófoli, Giovana Radomille
Campos, Estefânia Vangelie Ramos
Machado, Ian Pompermayer
Fraceto, Leonardo Fernandes
de Sairre, Mirela Inês
de Araujo, Daniele Ribeiro
Physico-Chemical Characterization and Biopharmaceutical Evaluation of Lipid-Poloxamer-Based Organogels for Curcumin Skin Delivery
title Physico-Chemical Characterization and Biopharmaceutical Evaluation of Lipid-Poloxamer-Based Organogels for Curcumin Skin Delivery
title_full Physico-Chemical Characterization and Biopharmaceutical Evaluation of Lipid-Poloxamer-Based Organogels for Curcumin Skin Delivery
title_fullStr Physico-Chemical Characterization and Biopharmaceutical Evaluation of Lipid-Poloxamer-Based Organogels for Curcumin Skin Delivery
title_full_unstemmed Physico-Chemical Characterization and Biopharmaceutical Evaluation of Lipid-Poloxamer-Based Organogels for Curcumin Skin Delivery
title_short Physico-Chemical Characterization and Biopharmaceutical Evaluation of Lipid-Poloxamer-Based Organogels for Curcumin Skin Delivery
title_sort physico-chemical characterization and biopharmaceutical evaluation of lipid-poloxamer-based organogels for curcumin skin delivery
topic Pharmacology
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6751402/
https://www.ncbi.nlm.nih.gov/pubmed/31572185
http://dx.doi.org/10.3389/fphar.2019.01006
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