Abstract
The absorption modulating activity of two alkylglycerol derivatives (batyl and chimyl alcohol) on skin barrier properties was evaluated. Biophysical tests such as transepidermal water loss (TEWL) and attenuated total reflectance–Fourier transform infrared (ATR-FTIR) spectroscopy, as well as in vitro skin permeation studies, were performed in order to determine the effect of these compounds as chemical absorption modulators. Four drugs were used as models: three NSAIDS (diclofenac, naproxen, and piroxicam) and glycyrrhizic acid. The results showed that treatment of the skin with alkylglycerols caused (i) a reduction on the amount of drug permeated; (ii) a reduction in TEWL; and (iii) changes in the ATR-FTIR peaks of stratum corneum lipids, indicative of a more ordered structure. All of these findings confirm that alkyl glycerols have an absorption retarding effect on the drugs tested. Such effects are expected to give rise to important applications in the pharmaceutical and cosmetic sectors, in cases where it is desirable for the drug to remain in the superficial layers of the skin to achieve a local effect.
Highlights
It is fully recognized that one of the major drawbacks when administering drugs through the skin, especially when seeking a systemic effect, is the limited permeation of most of these drugs due to the presence of the barrier imposed by the structural characteristics of the stratum corneum (SC) [1]
These molecules known as penetration retarders or reducers, may be useful by restricting the location of the drugs to the uppermost layers of the skin, in those cases where the target site is the surface of the skin, and when absorption may lead to unwanted side effects or toxicity
A reduction in the amount of diclofenac, naproxen, and glycyrrhizic was feature is that similar profiles withwith fluxthe values close to each were obtained thefeature two AG
Summary
It is fully recognized that one of the major drawbacks when administering drugs through the skin, especially when seeking a systemic effect, is the limited permeation of most of these drugs due to the presence of the barrier imposed by the structural characteristics of the stratum corneum (SC) [1]. While some penetration enhancers act on skin lipids, creating a more fluid environment and promoting therapeutic agents to permeate, there are molecules with an opposite effect [4] These molecules known as penetration retarders or reducers, may be useful by restricting the location of the drugs to the uppermost layers of the skin, in those cases where the target site is the surface of the skin, and when absorption may lead to unwanted side effects or toxicity. Both enhancers and retarders are known as penetration modifiers [5]. The mechanisms of action of retarders have not been completely understood, Molecules 2017, 22, 185; doi:10.3390/molecules22010185 www.mdpi.com/journal/molecules
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