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Amphiphilic transdermal permeation enhancers: structure-activity relationships.
TLDR
An overview of the methods used for investigation of the mechanisms of permeation enhancement, namely differential scanning calorimetry (DSC), infrared (IR) and Raman spectroscopy, X-ray diffraction and future perspectives in this field are given.
Dimethylamino Acid Esters as Biodegradable and Reversible Transdermal Permeation Enhancers: Effects of Linking Chain Length, Chirality and Polyfluorination
TLDR
DDAK, highly effective, broad-spectrum, biodegradable and reversible transdermal permeation enhancer, is promising candidate for future research.
Permeation enhancer dodecyl 6-(dimethylamino)hexanoate increases transdermal and topical delivery of adefovir: influence of pH, ion-pairing and skin species.
TLDR
The effect of permeation enhancer DDAK (6-dimethylaminohexanoic acid dodecyl ester) on the transdermal and topical delivery of adefovir and other acyclic nucleoside phosphonates offers an attractive alternative to established routes of administration.
S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
TLDR
The analogues with a trifluoromethyl group instead of one of the nitro groups maintained a high antimycobacterial activity, which indicates the possibility for further structural optimization of this class of antitubercular agents.
Ceramides in the skin lipid membranes: length matters.
TLDR
The model skin lipid membranes are a valuable tool to study the relationships between the lipid structure and composition, lipid organization, and the membrane permeability, and long acyl chains in ceramides are essential for the formation of tightly packed impermeable lipid lamellae.
Effect of ceramide acyl chain length on skin permeability and thermotropic phase behavior of model stratum corneum lipid membranes.
TLDR
The long hydrophobic chains in the NS-type ceramides are essential for maintaining the skin barrier function, however, this ability is not shared by their short-chain counterparts despite their having the same polar head structure and hydrogen bonding ability.
Short-Chain Ceramides Decrease Skin Barrier Properties
TLDR
The relationship between ceramide acyl chain length and its ability to perturb skin barrier showed striking similarity to the behavior of short- chain ceramides in sphingomyelin/phospholipid membranes and confirmed that short-chain ceramide do not act as natural ceramided and their use as experimental tools should be cautious.
1-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant
TLDR
Relatively high variability of substituent R(1) on the tetrazole in the absence of negative effects on antimycobacterial activity allows further structural optimization with respect to toxicity and the ADME properties of the 1-substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles lead compounds.
Synthetic ceramide analogues as skin permeation enhancers: structure-activity relationships.
TLDR
This finding confirms the Warner's hypothesis that the polar head of an enhancer is responsible for the permeation and anchoring of the molecule into the stratum corneum lipids and that it does not influence the mechanism of action.
Biodegradable derivatives of tranexamic acid as transdermal permeation enhancers.
TLDR
Biodegradable enhancers of this type could mediate easier and faster recovery of the skin barrier after transdermal delivery through the action of the released TXA, which was previously shown to improve skin barrier homeostasis.
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