Cargando…
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...
Autores principales: | , , , , , , , , , , , |
---|---|
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 |
_version_ | 1783452615167705088 |
---|---|
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. |
format | Online Article Text |
id | pubmed-6751402 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT vigatoaryanealves physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery AT querobinosamyrmachado physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery AT defarianaiallycardoso physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery AT candidoanacarolinabolelabovo physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery AT magalhaeslizandraguidi physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery AT ceredacintiamariasaia physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery AT tofoligiovanaradomille physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery AT camposestefaniavangelieramos physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery AT machadoianpompermayer physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery AT fracetoleonardofernandes physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery AT desairremirelaines physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery AT dearaujodanieleribeiro physicochemicalcharacterizationandbiopharmaceuticalevaluationoflipidpoloxamerbasedorganogelsforcurcuminskindelivery |