Positively Charged Lipid as Potential Tool to Influence the Fate of Ethosomes

Ethosomes<sup>®</sup> are one of the main deformable vesicles proposed to overcome the stratum corneum. They are composed of lecithin, ethanol and water, resulting in round vesicles characterized by a narrow size distribution and a negative surface charge. Taking into account their effic...

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Main Authors: Antonia Mancuso, Maria Chiara Cristiano, Massimo Fresta, Daniele Torella, Donatella Paolino
Format: Article
Language:English
Published: MDPI AG 2021-07-01
Series:Applied Sciences
Subjects:
Online Access:https://www.mdpi.com/2076-3417/11/15/7060
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author Antonia Mancuso
Maria Chiara Cristiano
Massimo Fresta
Daniele Torella
Donatella Paolino
author_facet Antonia Mancuso
Maria Chiara Cristiano
Massimo Fresta
Daniele Torella
Donatella Paolino
author_sort Antonia Mancuso
collection DOAJ
description Ethosomes<sup>®</sup> are one of the main deformable vesicles proposed to overcome the stratum corneum. They are composed of lecithin, ethanol and water, resulting in round vesicles characterized by a narrow size distribution and a negative surface charge. Taking into account their efficiency to deliver drugs into deeper skin layers, the current study was designed to evaluate the influence of different lipids on the physico-chemical features of traditional ethosomes in the attempt to influence their fate. Three lipids (DOPE, DSPE and DOTAP) were used for the study, but only DOTAP conferred a net positive charge to ethosomes, maintaining a narrow mean size lower than 300 nm and a good polydispersity index. Stability and in vitro cytotoxic studies have been performed using Turbiscan Lab analysis and MTT dye exclusion assay, respectively. Data recorded demonstrated the good stability of modified ethosomes and a reasonable absence of cell mortality when applied to human keratinocytes, NCTC 2544, which are used as a cell model. Finally, the best formulations were selected to evaluate their ability to encapsulate drugs, through the use of model compounds. Cationic ethosomes encapsulated oil red o and rhodamine b in amounts comparable to those recorded from conventional ethosomes (over 50%). Results recorded from this study are encouraging as cationic ethosomes may open new opportunities for skin delivery.
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spelling doaj.art-6e068d1f8922408392b30a94c4151a392023-11-22T05:23:47ZengMDPI AGApplied Sciences2076-34172021-07-011115706010.3390/app11157060Positively Charged Lipid as Potential Tool to Influence the Fate of EthosomesAntonia Mancuso0Maria Chiara Cristiano1Massimo Fresta2Daniele Torella3Donatella Paolino4Department of Health Science, Campus Universitario–Germaneto, University “Magna Græcia” of Catanzaro, Viale Europa, 88100 Catanzaro, ItalyDepartment of Experimental and Clinical Medicine, Campus Universitario–Germaneto, University “Magna Græcia” of Catanzaro, Viale Europa, 88100 Catanzaro, ItalyDepartment of Health Science, Campus Universitario–Germaneto, University “Magna Græcia” of Catanzaro, Viale Europa, 88100 Catanzaro, ItalyDepartment of Experimental and Clinical Medicine, Campus Universitario–Germaneto, University “Magna Græcia” of Catanzaro, Viale Europa, 88100 Catanzaro, ItalyDepartment of Experimental and Clinical Medicine, Campus Universitario–Germaneto, University “Magna Græcia” of Catanzaro, Viale Europa, 88100 Catanzaro, ItalyEthosomes<sup>®</sup> are one of the main deformable vesicles proposed to overcome the stratum corneum. They are composed of lecithin, ethanol and water, resulting in round vesicles characterized by a narrow size distribution and a negative surface charge. Taking into account their efficiency to deliver drugs into deeper skin layers, the current study was designed to evaluate the influence of different lipids on the physico-chemical features of traditional ethosomes in the attempt to influence their fate. Three lipids (DOPE, DSPE and DOTAP) were used for the study, but only DOTAP conferred a net positive charge to ethosomes, maintaining a narrow mean size lower than 300 nm and a good polydispersity index. Stability and in vitro cytotoxic studies have been performed using Turbiscan Lab analysis and MTT dye exclusion assay, respectively. Data recorded demonstrated the good stability of modified ethosomes and a reasonable absence of cell mortality when applied to human keratinocytes, NCTC 2544, which are used as a cell model. Finally, the best formulations were selected to evaluate their ability to encapsulate drugs, through the use of model compounds. Cationic ethosomes encapsulated oil red o and rhodamine b in amounts comparable to those recorded from conventional ethosomes (over 50%). Results recorded from this study are encouraging as cationic ethosomes may open new opportunities for skin delivery.https://www.mdpi.com/2076-3417/11/15/7060ethosomescationic ethosomesdrug delivery systemssurface chargecutaneous administration
spellingShingle Antonia Mancuso
Maria Chiara Cristiano
Massimo Fresta
Daniele Torella
Donatella Paolino
Positively Charged Lipid as Potential Tool to Influence the Fate of Ethosomes
Applied Sciences
ethosomes
cationic ethosomes
drug delivery systems
surface charge
cutaneous administration
title Positively Charged Lipid as Potential Tool to Influence the Fate of Ethosomes
title_full Positively Charged Lipid as Potential Tool to Influence the Fate of Ethosomes
title_fullStr Positively Charged Lipid as Potential Tool to Influence the Fate of Ethosomes
title_full_unstemmed Positively Charged Lipid as Potential Tool to Influence the Fate of Ethosomes
title_short Positively Charged Lipid as Potential Tool to Influence the Fate of Ethosomes
title_sort positively charged lipid as potential tool to influence the fate of ethosomes
topic ethosomes
cationic ethosomes
drug delivery systems
surface charge
cutaneous administration
url https://www.mdpi.com/2076-3417/11/15/7060
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