Investigation of Permeation of Theophylline through Skin Using Selected Piperazine-2,5-Diones

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F86652079%3A_____%2F19%3A00551751" target="_blank" >RIV/86652079:_____/19:00551751 - isvavai.cz</a>

Alternative codes found

RIV/68081715:_____/19:00501091 RIV/86652079:_____/19:00501091 RIV/61989592:15310/19:73596642 RIV/62157124:16370/19:43877852

Result on the web

<a href="https://www.mdpi.com/1420-3049/24/3/566" target="_blank" >https://www.mdpi.com/1420-3049/24/3/566</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/molecules24030566" target="_blank" >10.3390/molecules24030566</a>

Result language

angličtina

Original language name

Investigation of Permeation of Theophylline through Skin Using Selected Piperazine-2,5-Diones

Original language description

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 Withdrawn samples were analyzed by RP-HPLC for determination of the permeated amount of theophylline.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.

Czech name

—

Czech description

—

Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

10608 - Biochemistry and molecular biology

Project

<a href="/en/project/LO1415" target="_blank" >LO1415: CzechGlobe 2020 – Development of the Centre of Global Climate Change Impacts Studies</a><br>

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2019

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Molecules

ISSN

1420-3049

e-ISSN

1420-3049

Volume of the periodical

24

Issue of the periodical within the volume

3

Country of publishing house

CH - SWITZERLAND

Number of pages

14

Pages from-to

566

UT code for WoS article

000458934000190

EID of the result in the Scopus database

2-s2.0-85061058020