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首页> 外文期刊>BMC Veterinary Research >The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin
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The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin

机译：化学和物理渗透促进剂对利多卡因经马皮经皮渗透的影响

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Background The 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. Results All 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. Conclusion Microneedles represent a promising tool for transdermal lidocaine application in the horse with a rapid systemic bioavailability.
机译：背景技术在马匹中研究了物理和化学渗透促进剂对利多卡因体外透皮渗透的影响。因此，检查了六种媒介物（磷酸盐缓冲液（PBS），50％乙醇，50％丙二醇，50％异丙醇，50％异丙醇/肉豆蔻酸异丙酯和50％二甲亚砜）的效果，以及使用利多卡因透皮给药的不同针长。该皮肤是从六只Warmblood马的胸腔中获得的，并在-20°C下保存长达两周。 Franz型扩散池用于研究​​皮肤裂口（厚度600？μm）的透皮渗透性。受体液中利多卡因的含量通过UV-VIS高效液相色谱法测定。结果与除二甲基亚砜以外的纯PBS相比，所有研究的赋形剂补充剂均降低了利多卡因通过马皮肤的透皮通量，从而导致了与PBS相当的渗透率。在50％乙醇，丙二醇，异丙醇和异丙醇/肉豆蔻酸异丙酯中施用利多卡因的最大通量（J max ）低1.6-1.8倍。当将利多卡因以PBS的形式应用到经过微针预处理的皮肤上时，在两个针长上的渗透率相似，观察到的利多卡因的J max 明显更高。 6小时后，经微针预处理的皮肤样品的回收率比未处理的对照样品高1.7倍。在微针预处理的皮肤样品中，滞后时间减少到20–50％。结论微针代表了在马中经皮利多卡因应用的有前途的工具，具有快速的全身生物利用度。

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