The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin

BMC Veterinary Research

Manfred Kietzmann¹  Jessica Stahl¹ 

[1] Department of Pharmacology, Toxicology and Pharmacy, University of Veterinary Medicine Hannover, Foundation, Buenteweg 17, 30559, Hannover, Germany

关键词: Equine skin;    Microneedles;    Permeation enhancer;    Topical application;    Percutaneous Permeation;    Lidocaine;   

Others  :  866662
DOI  :  10.1186/1746-6148-10-138

 received in 2014-02-03, accepted in 2014-06-10,  发布年份 2014

【 摘 要 】

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 (J_max) was 1.6-1.8 fold lower for lidocaine applied in 50% ethanol, propylene glycol, isopropylalcohol and isopropylalcohol/isopropylmyristate. A significant higher J_max 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.

【 授权许可】

   
2014 Stahl and Kietzmann; licensee BioMed Central Ltd.

【 图 表 】

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