Daniela Monti, E. Egiziano, S. Burgalassi
2004
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Abstract
The aim of this study was to verify the effect of several cyclic onium based ionic liquids (ILs), including mono-and dicationic derivatives of 1,4-diazabicyclo[2.2.2]octane (DABCO), a dialkyl 15 morpholinium salt and a Brønsted acidic IL, as enhancers of the in vitro transdermal permeation and skin retention of diltiazem through and into hairless rat skin. The drug was used as both the hydrochloride salt (DZHCl) and the free base (DZB) to highlight the relationship between the enhancement effect and the physico-chemical characteristics of the active agent. Permeation tests were carried out using Gummer-type diffusion cells and excised rat skin with a 0.005 M aqueous 20 solution of diltiazem hydrochloride or diltiazem free base with and without the addition of 1% w/w ionic liquids. At the end of the permeation experiments with diltiazem hydrochloride, a suitable extraction procedure allowed for the determination of the drug content retained in the skin. Depending on the ionic liquid structure, a significant enhancement in diltiazem hydrochloride levels in the receiving phase was observed, and the transdermal permeation of the diltiazem free base was 25 markedly increased by treatment with all of the ionic liquids. N -dodecyldabco bromide was the best enhancer for both salified and free base