Simultaneous analysis of skin penetration of surfactant and active drug from fluorosurfactant-based microemulsions

[Display omitted] •Sensitive and specific 19F NMR for quantification of the fluorinated vehicle.•Simultaneous analysis of the vehicle component and active drug.•To set their penetration behaviour in relation, their relative slopes were calculated.•Microemulsion systems exerted a ‘push’ on drug skin...

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Veröffentlicht in:	European journal of pharmaceutics and biopharmaceutics Jg. 88; H. 1; S. 34 - 39
Hauptverfasser:	Mahrhauser, Denise, Hoppel, Magdalena, Schöll, Judith, Binder, Lisa, Kählig, Hanspeter, Valenta, Claudia
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	Netherlands Elsevier B.V 01.09.2014
Schlagworte:	19F NMR Animals ATR-FTIR Chromatography, High Pressure Liquid Diclofenac - chemistry Drug Delivery Systems Ear, External - drug effects Emulsions Fluorine Fluorosurfactant Lipids - chemistry Magnetic Resonance Spectroscopy Microemulsion Oleic Acid - chemistry Rheology Simultaneous analysis Skin - drug effects Skin Absorption Sodium - chemistry Spectroscopy, Fourier Transform Infrared Surface-Active Agents - administration & dosage Surface-Active Agents - chemistry Swine Vehicle penetration SC Fluorosurfactant ATR-FTIR Vehicle penetration ME SIN HEX Microemulsion FS Simultaneous analysis 19F NMR DS F NMR
ISSN:	0939-6411, 1873-3441, 1873-3441
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Abstract	[Display omitted] •Sensitive and specific 19F NMR for quantification of the fluorinated vehicle.•Simultaneous analysis of the vehicle component and active drug.•To set their penetration behaviour in relation, their relative slopes were calculated.•Microemulsion systems exerted a ‘push’ on drug skin penetration. The purpose of this study was to investigate the penetrated amount of the incorporated model drug diclofenac-sodium and of a fluorosurfactant as specific vehicle constituent of topically applied microemulsions at the same time. To this end, the penetration depth of each compound was elucidated through tape stripping studies by the simultaneous quantification of diclofenac-sodium and the fluorosurfactant from the same sample. A new approach was made by using the very sensitive and specific 19F NMR (nuclear magnetic resonance) for quantification of the fluorinated vehicle component. The tape stripping experiments with the microemulsions showed an almost similar penetration velocity of diclofenac-sodium and fluorosurfactant, suggesting that the surfactant within the microemulsion-structure intensified the stratum corneum uptake of the incorporated active constituent. Moreover, ATR-FTIR studies on porcine ear skin revealed significant shifts of the CH2 stretching absorbances, which are associated with an enhanced disorder of the SC lipids resulting in a decreased skin barrier function, after application of the microemulsions. However, the application of pure fluorosurfactant did not cause any shifts in the CH2 stretching absorbances. It can be thereby concluded that the prepared microemulsions exerted specific effects on skin integrity resulting in a “push” of diclofenac-sodium penetration.
AbstractList	The purpose of this study was to investigate the penetrated amount of the incorporated model drug diclofenac-sodium and of a fluorosurfactant as specific vehicle constituent of topically applied microemulsions at the same time. To this end, the penetration depth of each compound was elucidated through tape stripping studies by the simultaneous quantification of diclofenac-sodium and the fluorosurfactant from the same sample. A new approach was made by using the very sensitive and specific (19)F NMR (nuclear magnetic resonance) for quantification of the fluorinated vehicle component. The tape stripping experiments with the microemulsions showed an almost similar penetration velocity of diclofenac-sodium and fluorosurfactant, suggesting that the surfactant within the microemulsion-structure intensified the stratum corneum uptake of the incorporated active constituent. Moreover, ATR-FTIR studies on porcine ear skin revealed significant shifts of the CH₂ stretching absorbances, which are associated with an enhanced disorder of the SC lipids resulting in a decreased skin barrier function, after application of the microemulsions. However, the application of pure fluorosurfactant did not cause any shifts in the CH₂ stretching absorbances. It can be thereby concluded that the prepared microemulsions exerted specific effects on skin integrity resulting in a "push" of diclofenac-sodium penetration. The purpose of this study was to investigate the penetrated amount of the incorporated model drug diclofenac-sodium and of a fluorosurfactant as specific vehicle constituent of topically applied microemulsions at the same time. To this end, the penetration depth of each compound was elucidated through tape stripping studies by the simultaneous quantification of diclofenac-sodium and the fluorosurfactant from the same sample. A new approach was made by using the very sensitive and specific (19)F NMR (nuclear magnetic resonance) for quantification of the fluorinated vehicle component. The tape stripping experiments with the microemulsions showed an almost similar penetration velocity of diclofenac-sodium and fluorosurfactant, suggesting that the surfactant within the microemulsion-structure intensified the stratum corneum uptake of the incorporated active constituent. Moreover, ATR-FTIR studies on porcine ear skin revealed significant shifts of the CH₂ stretching absorbances, which are associated with an enhanced disorder of the SC lipids resulting in a decreased skin barrier function, after application of the microemulsions. However, the application of pure fluorosurfactant did not cause any shifts in the CH₂ stretching absorbances. It can be thereby concluded that the prepared microemulsions exerted specific effects on skin integrity resulting in a "push" of diclofenac-sodium penetration.The purpose of this study was to investigate the penetrated amount of the incorporated model drug diclofenac-sodium and of a fluorosurfactant as specific vehicle constituent of topically applied microemulsions at the same time. To this end, the penetration depth of each compound was elucidated through tape stripping studies by the simultaneous quantification of diclofenac-sodium and the fluorosurfactant from the same sample. A new approach was made by using the very sensitive and specific (19)F NMR (nuclear magnetic resonance) for quantification of the fluorinated vehicle component. The tape stripping experiments with the microemulsions showed an almost similar penetration velocity of diclofenac-sodium and fluorosurfactant, suggesting that the surfactant within the microemulsion-structure intensified the stratum corneum uptake of the incorporated active constituent. Moreover, ATR-FTIR studies on porcine ear skin revealed significant shifts of the CH₂ stretching absorbances, which are associated with an enhanced disorder of the SC lipids resulting in a decreased skin barrier function, after application of the microemulsions. However, the application of pure fluorosurfactant did not cause any shifts in the CH₂ stretching absorbances. It can be thereby concluded that the prepared microemulsions exerted specific effects on skin integrity resulting in a "push" of diclofenac-sodium penetration. [Display omitted] •Sensitive and specific 19F NMR for quantification of the fluorinated vehicle.•Simultaneous analysis of the vehicle component and active drug.•To set their penetration behaviour in relation, their relative slopes were calculated.•Microemulsion systems exerted a ‘push’ on drug skin penetration. The purpose of this study was to investigate the penetrated amount of the incorporated model drug diclofenac-sodium and of a fluorosurfactant as specific vehicle constituent of topically applied microemulsions at the same time. To this end, the penetration depth of each compound was elucidated through tape stripping studies by the simultaneous quantification of diclofenac-sodium and the fluorosurfactant from the same sample. A new approach was made by using the very sensitive and specific 19F NMR (nuclear magnetic resonance) for quantification of the fluorinated vehicle component. The tape stripping experiments with the microemulsions showed an almost similar penetration velocity of diclofenac-sodium and fluorosurfactant, suggesting that the surfactant within the microemulsion-structure intensified the stratum corneum uptake of the incorporated active constituent. Moreover, ATR-FTIR studies on porcine ear skin revealed significant shifts of the CH2 stretching absorbances, which are associated with an enhanced disorder of the SC lipids resulting in a decreased skin barrier function, after application of the microemulsions. However, the application of pure fluorosurfactant did not cause any shifts in the CH2 stretching absorbances. It can be thereby concluded that the prepared microemulsions exerted specific effects on skin integrity resulting in a “push” of diclofenac-sodium penetration.
Author	Mahrhauser, Denise Schöll, Judith Hoppel, Magdalena Binder, Lisa Kählig, Hanspeter Valenta, Claudia
Author_xml	– sequence: 1 givenname: Denise surname: Mahrhauser fullname: Mahrhauser, Denise organization: Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Vienna, Austria – sequence: 2 givenname: Magdalena surname: Hoppel fullname: Hoppel, Magdalena organization: Research Platform “Characterisation of Drug Delivery Systems on Skin and Investigations of Involved Mechanisms”, University of Vienna, Vienna, Austria – sequence: 3 givenname: Judith surname: Schöll fullname: Schöll, Judith organization: Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Vienna, Austria – sequence: 4 givenname: Lisa surname: Binder fullname: Binder, Lisa organization: Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Vienna, Austria – sequence: 5 givenname: Hanspeter surname: Kählig fullname: Kählig, Hanspeter organization: Research Platform “Characterisation of Drug Delivery Systems on Skin and Investigations of Involved Mechanisms”, University of Vienna, Vienna, Austria – sequence: 6 givenname: Claudia surname: Valenta fullname: Valenta, Claudia email: claudia.valenta@univie.ac.at organization: Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Vienna, Austria
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Copyright	2014 Elsevier B.V. Copyright © 2014 Elsevier B.V. All rights reserved.
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Keywords	SC Fluorosurfactant ATR-FTIR Vehicle penetration ME SIN HEX Microemulsion FS Simultaneous analysis 19F NMR DS F NMR
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Snippet	[Display omitted] •Sensitive and specific 19F NMR for quantification of the fluorinated vehicle.•Simultaneous analysis of the vehicle component and active... The purpose of this study was to investigate the penetrated amount of the incorporated model drug diclofenac-sodium and of a fluorosurfactant as specific...
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SubjectTerms	19F NMR Animals ATR-FTIR Chromatography, High Pressure Liquid Diclofenac - chemistry Drug Delivery Systems Ear, External - drug effects Emulsions Fluorine Fluorosurfactant Lipids - chemistry Magnetic Resonance Spectroscopy Microemulsion Oleic Acid - chemistry Rheology Simultaneous analysis Skin - drug effects Skin Absorption Sodium - chemistry Spectroscopy, Fourier Transform Infrared Surface-Active Agents - administration & dosage Surface-Active Agents - chemistry Swine Vehicle penetration
Title	Simultaneous analysis of skin penetration of surfactant and active drug from fluorosurfactant-based microemulsions
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