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
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Acceso en línea:https://doaj.org/article/144d7e5965b542cfa010b0e7e661aa1b
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Sumario: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.