N-Alkylmorpholines: Potent Dermal and Transdermal Skin Permeation Enhancers

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22310%2F21%3A43922383" target="_blank" >RIV/60461373:22310/21:43922383 - isvavai.cz</a>

Alternative codes found

RIV/60461373:22330/21:43922383 RIV/60461373:22340/21:43922383

Result on the web

<a href="https://www.mdpi.com/1999-4923/14/1/64/htm" target="_blank" >https://www.mdpi.com/1999-4923/14/1/64/htm</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/pharmaceutics14010064" target="_blank" >10.3390/pharmaceutics14010064</a>

Result language

angličtina

Original language name

N-Alkylmorpholines: Potent Dermal and Transdermal Skin Permeation Enhancers

Original language description

Transdermal drug delivery is an attractive non-invasive method offering numerous advantages over the conventional routes of administration. The main obstacle to drug transport is, however, the powerful skin barrier that needs to be modulated, for example, by transdermal permeation enhancers. Unfortunately, there are still only a few enhancers showing optimum properties including low toxicity and reversibility of enhancing effects. For this reason, we investigated a series of new N-alkylmorpholines with various side chains as potential enhancers in an in vitro permeation study, using three model permeants (theophylline, indomethacin, diclofenac). Moreover, electrical impedance, transepidermal water loss, cellular toxicity and infrared spectroscopy measurements were applied to assess the effect of enhancers on skin integrity, reversibility, toxicity and enhancers’ mode of action, respectively. Our results showed a bell-shaped relationship between the enhancing activity and the hydrocarbon chain length of the N-alkylmorpholines, with the most efficient derivatives having 10–14 carbons for both transdermal and dermal delivery. These structures were even more potent than the unsaturated oleyl derivative. The best results were obtained for indomethacin, where particularly the C10-14 derivatives showed significantly stronger effects than the traditional enhancer Azone. Further experiments revealed reversibility in the enhancing effect, acceptable toxicity and a mode of action based predominantly on interactions with stratum corneum lipids.

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

30104 - Pharmacology and pharmacy

Project

<a href="/en/project/GA19-09600S" target="_blank" >GA19-09600S: Integrated design methodology of nanoformulation processes for (trans-)dermal delivery of actives</a><br>

Continuities

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

Publication year

2021

Confidentiality

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

Name of the periodical

PHARMACEUTICS

ISSN

1999-4923

e-ISSN

—

Volume of the periodical

14

Issue of the periodical within the volume

1

Country of publishing house

CH - SWITZERLAND

Number of pages

16

Pages from-to

64

UT code for WoS article

000757393200001

EID of the result in the Scopus database

2-s2.0-85122163389