Assessment of the Effect of Structural Modification of Ibuprofen on the Penetration of Ibuprofen from Pentravan<sup>®</sup> (Semisolid) Formulation Using Human Skin and a Transdermal Diffusion Test Model

The effect of transdermal vehicle (Pentravan<sup>®</sup>) on skin permeability was examined for unmodified ibuprofen (IBU) and ion pairs of ibuprofen with new L-valine alkyl esters [ValOR][IBU]. The percutaneous permeation across the human skin and transdermal diffusion test model (Strat...

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Autores principales:	Paula Ossowicz-Rupniewska, Anna Nowak, Joanna Klebeko, Ewa Janus, Wiktoria Duchnik, Urszula Adamiak-Giera, Łukasz Kucharski, Piotr Prowans, Jan Petriczko, Norbert Czapla, Piotr Bargiel, Marta Markowska, Adam Klimowicz
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	structural modification of ibuprofen increasing drug permeability Franz cell diffusion transdermal delivery system Pentravan<sup>®</sup> human skin Technology T Electrical engineering. Electronics. Nuclear engineering TK1-9971 Engineering (General). Civil engineering (General) TA1-2040 Microscopy QH201-278.5 Descriptive and experimental mechanics QC120-168.85
Acceso en línea:	https://doaj.org/article/144d7e5965b542cfa010b0e7e661aa1b
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spelling	oai:doaj.org-article:144d7e5965b542cfa010b0e7e661aa1b2021-11-25T18:13:45ZAssessment of the Effect of Structural Modification of Ibuprofen on the Penetration of Ibuprofen from Pentravan<sup>®</sup> (Semisolid) Formulation Using Human Skin and a Transdermal Diffusion Test Model10.3390/ma142268081996-1944https://doaj.org/article/144d7e5965b542cfa010b0e7e661aa1b2021-11-01T00:00:00Zhttps://www.mdpi.com/1996-1944/14/22/6808https://doaj.org/toc/1996-1944The effect of transdermal vehicle (Pentravan<sup>®</sup>) on skin permeability was examined for unmodified ibuprofen (IBU) and ion pairs of ibuprofen with new L-valine alkyl esters [ValOR][IBU]. The percutaneous permeation across the human skin and transdermal diffusion test model (Strat-M<sup>®</sup> membranes) of ibuprofen and its structural modification were measured and compared using Franz diffusion cells. For comparison, the penetration of ibuprofen from a commercial product was also investigated. The cumulative amount of drug permeated through human skin at the end of the 24 h study was highest for ibuprofen derivatives containing propyl (C3), isopropyl (C3), ethyl (C2), and butyl (C4) esters. For Strat-M<sup>®</sup>, the best results were obtained with the alkyl chain length of the ester from C2 to C5. The permeation profiles and parameters were appointed, such as steady-state flux, lag time, and permeability coefficient. It has been shown that L-valine alkyl ester ibuprofenates, with the propyl, butyl, and amyl chain, exhibit a higher permeation rate than ibuprofen. The diffusion parameters of analyzed drugs through human skin and Strat-M<sup>®</sup> were similar and with good correlation. The resulting Pentravan-based creams with ibuprofen in the form of an ionic pair represent a potential alternative to other forms of the drug-containing analgesics administered transdermally. Furthermore, the Strat-M<sup>®</sup> membranes can be used to assess the permeation of transdermal preparations containing anti-inflammatory drugs.Paula Ossowicz-RupniewskaAnna NowakJoanna KlebekoEwa JanusWiktoria DuchnikUrszula Adamiak-GieraŁukasz KucharskiPiotr ProwansJan PetriczkoNorbert CzaplaPiotr BargielMarta MarkowskaAdam KlimowiczMDPI AGarticlestructural modification of ibuprofenincreasing drug permeabilityFranz cell diffusiontransdermal delivery systemPentravan<sup>®</sup>human skinTechnologyTElectrical engineering. Electronics. Nuclear engineeringTK1-9971Engineering (General). Civil engineering (General)TA1-2040MicroscopyQH201-278.5Descriptive and experimental mechanicsQC120-168.85ENMaterials, Vol 14, Iss 6808, p 6808 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	structural modification of ibuprofen increasing drug permeability Franz cell diffusion transdermal delivery system Pentravan<sup>®</sup> human skin Technology T Electrical engineering. Electronics. Nuclear engineering TK1-9971 Engineering (General). Civil engineering (General) TA1-2040 Microscopy QH201-278.5 Descriptive and experimental mechanics QC120-168.85
spellingShingle	structural modification of ibuprofen increasing drug permeability Franz cell diffusion transdermal delivery system Pentravan<sup>®</sup> human skin Technology T Electrical engineering. Electronics. Nuclear engineering TK1-9971 Engineering (General). Civil engineering (General) TA1-2040 Microscopy QH201-278.5 Descriptive and experimental mechanics QC120-168.85 Paula Ossowicz-Rupniewska Anna Nowak Joanna Klebeko Ewa Janus Wiktoria Duchnik Urszula Adamiak-Giera Łukasz Kucharski Piotr Prowans Jan Petriczko Norbert Czapla Piotr Bargiel Marta Markowska Adam Klimowicz Assessment of the Effect of Structural Modification of Ibuprofen on the Penetration of Ibuprofen from Pentravan<sup>®</sup> (Semisolid) Formulation Using Human Skin and a Transdermal Diffusion Test Model
description	The effect of transdermal vehicle (Pentravan<sup>®</sup>) on skin permeability was examined for unmodified ibuprofen (IBU) and ion pairs of ibuprofen with new L-valine alkyl esters [ValOR][IBU]. The percutaneous permeation across the human skin and transdermal diffusion test model (Strat-M<sup>®</sup> membranes) of ibuprofen and its structural modification were measured and compared using Franz diffusion cells. For comparison, the penetration of ibuprofen from a commercial product was also investigated. The cumulative amount of drug permeated through human skin at the end of the 24 h study was highest for ibuprofen derivatives containing propyl (C3), isopropyl (C3), ethyl (C2), and butyl (C4) esters. For Strat-M<sup>®</sup>, the best results were obtained with the alkyl chain length of the ester from C2 to C5. The permeation profiles and parameters were appointed, such as steady-state flux, lag time, and permeability coefficient. It has been shown that L-valine alkyl ester ibuprofenates, with the propyl, butyl, and amyl chain, exhibit a higher permeation rate than ibuprofen. The diffusion parameters of analyzed drugs through human skin and Strat-M<sup>®</sup> were similar and with good correlation. The resulting Pentravan-based creams with ibuprofen in the form of an ionic pair represent a potential alternative to other forms of the drug-containing analgesics administered transdermally. Furthermore, the Strat-M<sup>®</sup> membranes can be used to assess the permeation of transdermal preparations containing anti-inflammatory drugs.
format	article
author	Paula Ossowicz-Rupniewska Anna Nowak Joanna Klebeko Ewa Janus Wiktoria Duchnik Urszula Adamiak-Giera Łukasz Kucharski Piotr Prowans Jan Petriczko Norbert Czapla Piotr Bargiel Marta Markowska Adam Klimowicz
author_facet	Paula Ossowicz-Rupniewska Anna Nowak Joanna Klebeko Ewa Janus Wiktoria Duchnik Urszula Adamiak-Giera Łukasz Kucharski Piotr Prowans Jan Petriczko Norbert Czapla Piotr Bargiel Marta Markowska Adam Klimowicz
author_sort	Paula Ossowicz-Rupniewska
title	Assessment of the Effect of Structural Modification of Ibuprofen on the Penetration of Ibuprofen from Pentravan<sup>®</sup> (Semisolid) Formulation Using Human Skin and a Transdermal Diffusion Test Model
title_short	Assessment of the Effect of Structural Modification of Ibuprofen on the Penetration of Ibuprofen from Pentravan<sup>®</sup> (Semisolid) Formulation Using Human Skin and a Transdermal Diffusion Test Model
title_full	Assessment of the Effect of Structural Modification of Ibuprofen on the Penetration of Ibuprofen from Pentravan<sup>®</sup> (Semisolid) Formulation Using Human Skin and a Transdermal Diffusion Test Model
title_fullStr	Assessment of the Effect of Structural Modification of Ibuprofen on the Penetration of Ibuprofen from Pentravan<sup>®</sup> (Semisolid) Formulation Using Human Skin and a Transdermal Diffusion Test Model
title_full_unstemmed	Assessment of the Effect of Structural Modification of Ibuprofen on the Penetration of Ibuprofen from Pentravan<sup>®</sup> (Semisolid) Formulation Using Human Skin and a Transdermal Diffusion Test Model
title_sort	assessment of the effect of structural modification of ibuprofen on the penetration of ibuprofen from pentravan<sup>®</sup> (semisolid) formulation using human skin and a transdermal diffusion test model
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/144d7e5965b542cfa010b0e7e661aa1b
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Assessment of the Effect of Structural Modification of Ibuprofen on the Penetration of Ibuprofen from Pentravan<sup>®</sup> (Semisolid) Formulation Using Human Skin and a Transdermal Diffusion Test Model

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