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Home / Equine Research Bank / BMC Vet Res / The effects of chemical and physical penetration enhancers o...
BMC veterinary research2014; 10; 138; doi: 10.1186/1746-6148-10-138

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

Abstract: 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. Conclusions: Microneedles represent a promising tool for transdermal lidocaine application in the horse with a rapid systemic bioavailability.
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Publication Date: 2014-06-20 PubMed ID: 24950611PubMed Central: PMC4078091DOI: 10.1186/1746-6148-10-138Google Scholar: Lookup
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  • Journal Article

Summary

This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.

The research investigates the impact of chemical and physical permeation enhancers on the transdermal transfer of lidocaine in horse skin. Results showed that all tested carriers, except dimethylsulfoxide, reduced the transdermal flux of lidocaine compared to pure phosphate-buffered saline, while microneedles boosted lidocaine permeation.

Research Methodology

  • The researchers tested six different vehicles: phosphate-buffered saline, ethanol (50% concentration), propylene glycol (50% concentration), isopropyl alcohol (50% concentration), a mixture of isopropyl alcohol and isopropyl myristate (50% concentration), and dimethyl sulfoxide (50% concentration). They applied these on the skin of six Warmblood horses to see how they would affect the permeation of lidocaine.
  • The effects of microneedle pretreatment, using different needle lengths, on the transdermal delivery of lidocaine were also studied.
  • To conduct these studies, they used Franz-type diffusion cells, which allow them to track the amount of a drug that passes through a thin layer of skin. They took samples of the skin from the thorax of the horses and stored these at -20 degrees Celsius for up to two weeks.
  • The thickness of the split skin used was 600 μm. The dosage of lidocaine in the receptor fluid was tracked using UV-VIS high-performance liquid chromatography.

Findings

  • All examined vehicle supplements reduced the transdermal flux of lidocaine through equine skin in comparison to pure phosphate-buffered saline. The notable exception was dimethyl sulfoxide, which displayed comparable permeation rates with the saline.
  • The maximum flux of lidocaine was 1.6-1.8 times lower when using 50% concentrations of ethanol, propylene glycol, isopropyl alcohol, and the isopropyl alcohol/isopropyl myristate mixture.
  • The use of microneedles significantly increased the transdermal delivery of lidocaine, with the rate of permeation being similar regardless of the needle’s length. Six hours post-application, 1.7 times higher recovery rates were observed in samples that had undergone microneedle pretreatment compared to the untreated control samples.
  • The lag times, or the time it took for the drug to start permeating the skin, was reduced to 20-50% in the microneedle pretreated skin samples.

Conclusion

  • As a result of the study, the authors concluded that microneedles provide a promising tool for enhancing the effectiveness of transdermal lidocaine application in horses, and enable quicker systemic bioavailability of the drug.

Cite This Article

APA
Stahl J, Kietzmann M. (2014). The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin. BMC Vet Res, 10, 138. https://doi.org/10.1186/1746-6148-10-138

Publication

BMC veterinary research
ISSN: 1746-6148
NlmUniqueID: 101249759
Country: England
Language: English
Volume: 10
Pages: 138

Researcher Affiliations

Stahl, Jessica
  • Department of Pharmacology, Toxicology and Pharmacy, University of Veterinary Medicine Hannover, Foundation, Buenteweg 17, 30559, Hannover, Germany. Jessica.stahl@tiho-hannover.de.
Kietzmann, Manfred

    MeSH Terms

    • Administration, Cutaneous
    • Animals
    • Chemistry, Pharmaceutical
    • Drug Delivery Systems / methods
    • Horses
    • In Vitro Techniques
    • Lidocaine / pharmacokinetics
    • Permeability
    • Pharmaceutical Vehicles / pharmacology
    • Skin / drug effects
    • Skin Absorption / drug effects

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    Citations

    This article has been cited 5 times.
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    2. Alkilani AZ, Nasereddin J, Hamed R, Nimrawi S, Hussein G, Abo-Zour H, Donnelly RF. Beneath the Skin: A Review of Current Trends and Future Prospects of Transdermal Drug Delivery Systems. Pharmaceutics 2022 May 28;14(6).
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    4. Weber LA, Funtan A, Paschke R, Delarocque J, Kalbitz J, Meißner J, Feige K, Kietzmann M, Cavalleri JV. In vitro assessment of triterpenoids NVX-207 and betulinyl-bis-sulfamate as a topical treatment for equine skin cancer. PLoS One 2020;15(11):e0241448.
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