Permeability of Ibuprofen in the Form of Free Acid and Salts of L-Valine Alkyl Esters from a Hydrogel Formulation through Strat-M™ Membrane and Human Skin
This paper aimed to evaluate the effect of vehicle and chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU]. In vitro permeation experiments were performed using human abdominal skin and Strat-M™ membrane. The HPLC method was used for...
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MDPI AG
2021
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oai:doaj.org-article:9472320cd1e14397b6067c060486a7d02021-11-11T18:11:23ZPermeability of Ibuprofen in the Form of Free Acid and Salts of L-Valine Alkyl Esters from a Hydrogel Formulation through Strat-M™ Membrane and Human Skin10.3390/ma142166781996-1944https://doaj.org/article/9472320cd1e14397b6067c060486a7d02021-11-01T00:00:00Zhttps://www.mdpi.com/1996-1944/14/21/6678https://doaj.org/toc/1996-1944This paper aimed to evaluate the effect of vehicle and chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU]. In vitro permeation experiments were performed using human abdominal skin and Strat-M™ membrane. The HPLC method was used for quantitative determinations. The formulations tested were hydrogels containing IBU and its derivatives and commercial gel with ibuprofen. The results obtained indicate that Celugel<sup>®</sup> had an enhancing effect on the skin penetration of IBU. The average cumulative mass of [IBU] after 24 h permeation test from Celugel<sup>®</sup> formulation through human skin was over 3 times higher than for the commercial product. Three ibuprofen derivatives containing [ValOiPr][IBU], [ValOPr][IBU], and [ValOBu][IBU] cation were evaluated as chemical penetration enhancers. The cumulative mass after 24 h of penetration was 790.526 ± 41.426, 682.201 ± 29.910, and 684.538 ± 5.599 μg IBU cm<sup>−2</sup>, respectively, compared to the formulation containing unmodified IBU-429.672 ± 60.151 μg IBU cm<sup>−2</sup>. This study demonstrates the perspective of the transdermal hydrogel vehicle in conjunction with the modification of the drug as a potential faster drug delivery system.Joanna KlebekoPaula Ossowicz-RupniewskaAnna NowakEwa JanusWiktoria DuchnikUrszula Adamiak-GieraŁukasz KucharskiPiotr ProwansJan PetriczkoNorbert CzaplaPiotr BargielMarta MarkowskaAdam KlimowiczMDPI AGarticlederivatives of ibuprofenFranz cell diffusiontransdermal delivery systemCelugel<sup>®</sup>human skinStrat-M™TechnologyTElectrical engineering. Electronics. Nuclear engineeringTK1-9971Engineering (General). Civil engineering (General)TA1-2040MicroscopyQH201-278.5Descriptive and experimental mechanicsQC120-168.85ENMaterials, Vol 14, Iss 6678, p 6678 (2021) |
| institution |
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DOAJ |
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EN |
| topic |
derivatives of ibuprofen Franz cell diffusion transdermal delivery system Celugel<sup>®</sup> human skin Strat-M™ 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 |
derivatives of ibuprofen Franz cell diffusion transdermal delivery system Celugel<sup>®</sup> human skin Strat-M™ 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 Joanna Klebeko Paula Ossowicz-Rupniewska Anna Nowak Ewa Janus Wiktoria Duchnik Urszula Adamiak-Giera Łukasz Kucharski Piotr Prowans Jan Petriczko Norbert Czapla Piotr Bargiel Marta Markowska Adam Klimowicz Permeability of Ibuprofen in the Form of Free Acid and Salts of L-Valine Alkyl Esters from a Hydrogel Formulation through Strat-M™ Membrane and Human Skin |
| description |
This paper aimed to evaluate the effect of vehicle and chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU]. In vitro permeation experiments were performed using human abdominal skin and Strat-M™ membrane. The HPLC method was used for quantitative determinations. The formulations tested were hydrogels containing IBU and its derivatives and commercial gel with ibuprofen. The results obtained indicate that Celugel<sup>®</sup> had an enhancing effect on the skin penetration of IBU. The average cumulative mass of [IBU] after 24 h permeation test from Celugel<sup>®</sup> formulation through human skin was over 3 times higher than for the commercial product. Three ibuprofen derivatives containing [ValOiPr][IBU], [ValOPr][IBU], and [ValOBu][IBU] cation were evaluated as chemical penetration enhancers. The cumulative mass after 24 h of penetration was 790.526 ± 41.426, 682.201 ± 29.910, and 684.538 ± 5.599 μg IBU cm<sup>−2</sup>, respectively, compared to the formulation containing unmodified IBU-429.672 ± 60.151 μg IBU cm<sup>−2</sup>. This study demonstrates the perspective of the transdermal hydrogel vehicle in conjunction with the modification of the drug as a potential faster drug delivery system. |
| format |
article |
| author |
Joanna Klebeko Paula Ossowicz-Rupniewska Anna Nowak Ewa Janus Wiktoria Duchnik Urszula Adamiak-Giera Łukasz Kucharski Piotr Prowans Jan Petriczko Norbert Czapla Piotr Bargiel Marta Markowska Adam Klimowicz |
| author_facet |
Joanna Klebeko Paula Ossowicz-Rupniewska Anna Nowak Ewa Janus Wiktoria Duchnik Urszula Adamiak-Giera Łukasz Kucharski Piotr Prowans Jan Petriczko Norbert Czapla Piotr Bargiel Marta Markowska Adam Klimowicz |
| author_sort |
Joanna Klebeko |
| title |
Permeability of Ibuprofen in the Form of Free Acid and Salts of L-Valine Alkyl Esters from a Hydrogel Formulation through Strat-M™ Membrane and Human Skin |
| title_short |
Permeability of Ibuprofen in the Form of Free Acid and Salts of L-Valine Alkyl Esters from a Hydrogel Formulation through Strat-M™ Membrane and Human Skin |
| title_full |
Permeability of Ibuprofen in the Form of Free Acid and Salts of L-Valine Alkyl Esters from a Hydrogel Formulation through Strat-M™ Membrane and Human Skin |
| title_fullStr |
Permeability of Ibuprofen in the Form of Free Acid and Salts of L-Valine Alkyl Esters from a Hydrogel Formulation through Strat-M™ Membrane and Human Skin |
| title_full_unstemmed |
Permeability of Ibuprofen in the Form of Free Acid and Salts of L-Valine Alkyl Esters from a Hydrogel Formulation through Strat-M™ Membrane and Human Skin |
| title_sort |
permeability of ibuprofen in the form of free acid and salts of l-valine alkyl esters from a hydrogel formulation through strat-m™ membrane and human skin |
| publisher |
MDPI AG |
| publishDate |
2021 |
| url |
https://doaj.org/article/9472320cd1e14397b6067c060486a7d0 |
| work_keys_str_mv |
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