Investigation of permeation of theophylline through skin using selected piperazine-2,5-diones

0501091 - ÚIACH 2020 RIV CH eng J - Journal Article
Pokorná, A. - Bobáľ, P. - Oravec, Michal - Rárová, L. - Bobálová, Janette - Jampílek, J.
Investigation of permeation of theophylline through skin using selected piperazine-2,5-diones.
Molecules. Roč. 24, č. 3 (2019), č. článku 566. E-ISSN 1420-3049
R&D Projects: GA MŠMT(CZ) LO1415
Institutional support: RVO:68081715 ; RVO:86652079
Keywords : piperazine-2,5-diones * theophylline * permeation * HPLC * Franz diffusion cell
OECD category: Analytical chemistry; Analytical chemistry (UEK-B)
Impact factor: 3.267, year: 2019
Method of publishing: Open access
https://www.mdpi.com/1420-3049/24/3/566

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 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 Withdrawn samples were analyzed by RP-HPLC for determination of the permeated amount of theophylline.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.
Permanent Link: http://hdl.handle.net/11104/0293095