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Investigation of Permeation of Theophylline through Skin Using Selected Piperazine-2,5-Diones
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SYSNO ASEP 0551751 Document Type J - Journal Article R&D Document Type The record was not marked in the RIV Subsidiary J Článek ve WOS Title Investigation of Permeation of Theophylline through Skin Using Selected Piperazine-2,5-Diones Author(s) Pokorná, A. (CZ)
Bobál, P. (CZ)
Oravec, Michal (UEK-B) RID, ORCID, SAI
Rárová, L. (CZ)
Bobalová, J. (CZ)
Jampílek, J. (CZ)Number of authors 6 Year of issue 2019 Article number 566 Source Title Molecules. - : MDPI
Roč. 24, č. 3 (2019)Number of pages 14 s. Publication form Print - P Language eng - English Country CH - Switzerland Keywords penetration enhancers ; propylene-glycol ; ear skin ; delivery ; absorption ; model ; solubility ; dipeptides ; mechanism ; piperazine-2,5-diones ; theophylline ; permeation ; skin ; Franz diffusion cell ; HPLC determination ; cytotoxicity Subject RIV CE - Biochemistry OECD category Biochemistry and molecular biology R&D Projects LO1415 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Method of publishing Open access Institutional support UEK-B - RVO:86652079 UT WOS 000458934000190 EID SCOPUS 85061058020 DOI 10.3390/molecules24030566 Annotation Transdermal administration of drugs that penetrate, in this case directly into the blood circulation, has many advantages and is promising for many drugs thanks to its easy application and good patient compliance. (S)-8-Methyl-6,9-diazaspiro[4.5]decan-7,10-dione (alaptide), has been studied as a potential chemical permeation enhancer. Based on its structure, four selected piperazine-2,5-diones were synthesized by means of multi-step synthetic pathways. All the compounds were investigated on their ability to enhance the permeation of the model drug theophylline from the hydrophilic medium propylene glycol:water (1:1). In vitro experiments were performed using vertical Franz diffusion cells at constant temperature 34 +/- 0.5 degrees C and using full-thickness pig (Sus scrofa f. domestica) ear skin. Withdrawn samples were analyzed by RP-HPLC for determination of the permeated amount of theophylline. All the compounds were applied in ratio 1:10 (w/w) relative to the amount of theophylline. One hour after application, the permeated amount of theophylline from formulations with alaptide and (3S,6S)-3,6-dimethylpiperazine-2,5-dione, was ca. 15- and 12-fold higher, respectively, than from the formulation without the tested compounds. Despite the enhancement ratio of both enhancers in a steady state was ca. 2.3, the pseudo-enhancement ratio in the time range from 1 to 3 h was 4.4. These enhancement ratios indicate that the compounds are able to enhance the permeation of agents through the skin however, the short-term application of both compound formulations seems to be more advantageous. In addition, the screening of the cytotoxicity of all the prepared compounds was performed using three cell lines, and the compounds did not show any significant toxic effect. Workplace Global Change Research Institute Contact Nikola Šviková, svikova.n@czechglobe.cz, Tel.: 511 192 268 Year of Publishing 2022 Electronic address https://www.mdpi.com/1420-3049/24/3/566
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