Abstract
BackgroundThe effect of physical and chemical permeation enhancers on in vitro transdermal permeation of lidocaine was investigated in the horse.Therefore, the effect of six vehicles (phosphate-buffered saline (PBS), 50% ethanol, 50% propylene glycol, 50% isopropylalcohol, 50% isopropylalcohol/isopropylmyristate and 50% dimethylsulfoxide) was examined as well as the effect of microneedle pretreatment with different needle lengths on transdermal drug delivery of lidocaine.The skin was obtained from the thorax of six Warmblood horses and was stored up to two weeks at - 20°C. Franz-type diffusion cells were used to study the transdermal permeation through split skin (600 μm thickness). The amount of lidocaine in the receptor fluid was determined by UV–VIS high-performance liquid chromatography.ResultsAll investigated vehicle supplementations diminished the transdermal flux of lidocaine through equine skin in comparison to pure PBS except dimethylsulfoxide, which resulted in comparable permeation rates to PBS. The maximum flux (Jmax) was 1.6-1.8 fold lower for lidocaine applied in 50% ethanol, propylene glycol, isopropylalcohol and isopropylalcohol/isopropylmyristate. A significant higher Jmax of lidocaine was observed when lidocaine was applied in PBS onto microneedle pretreated skin with similar permeation rates in both needle lengths. After 6 hours, 1.7 fold higher recovery rates were observed in the microneedle pretreated skin samples than in the untreated control samples. The lagtimes were reduced to 20–50% in the microneedle pretreated skin samples.ConclusionMicroneedles represent a promising tool for transdermal lidocaine application in the horse with a rapid systemic bioavailability.
Highlights
The effect of physical and chemical permeation enhancers on in vitro transdermal permeation of lidocaine was investigated in the horse
Five different chemical additives known as permeation enhancers of transdermal drug delivery were investigated for their impact on transdermal lidocaine delivery through equine skin
The highest permeation of lidocaine was observed after administration of lidocaine in pure PBS and 50% DMSO
Summary
The effect of physical and chemical permeation enhancers on in vitro transdermal permeation of lidocaine was investigated in the horse. Lidocaine (lignocaine) represents an amide local anesthetic drug which is systemically used as an anti-arrhythmic drug [1]. It has recently gained interest as systemically used prokinetic drug in the treatment of the postoperative ileus in horses [2,3,4,5]. Five different chemical additives known as permeation enhancers of transdermal drug delivery (diemthylsulfoxide, ethanol, isopropylalcohol, isopropylmyristate and propylene glycol) were investigated for their impact on transdermal lidocaine delivery through equine skin. Physical penetration enhancement was performed using microneedles (200 μm and 300 μm long titanium needles) in order to pre-treat the equine skin samples before lidocaine application in the best aqueous solution determined in the first experimental setup
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