Microneedle pretreatment enhances the percutaneous permeation of hydrophilic compounds with high melting points

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• 作者：Jessica Stahl (1)
  Mareike Wohlert (1)
  Manfred Kietzmann (1)
  
• 关键词：Transdermal drug delivery ; Microneedles ; logKow ; Melting point ; Non ; steroidal anti ; inflammatory drug ; In vitro permeation study ; Physical penetration enhancement
• 刊名：BMC Pharmacology and Toxicology
• 出版年：2012
• 出版时间：December 2012
• 年：2012
• 卷：13
• 期：1
• 全文大小：440KB
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• 作者单位：Jessica Stahl (1)
  Mareike Wohlert (1)
  Manfred Kietzmann (1)
  
  1. Department of Pharmacology, Toxicology and Pharmacy, University of Veterinary Medicine Hannover, Foundation, Buenteweg 17, Hannover, 30559, Germany
  
• ISSN：2050-6511

文摘

Background Two commercially available microneedle rollers with a needle length of 200?μm and 300?μm were selected to examine the influence of microneedle pretreatment on the percutaneous permeation of four non-steroidal anti-inflammatory drugs (diclofenac, ibuprofen, ketoprofen, paracetamol) with different physicochemical drug characteristics in Franz-type diffusion cells. Samples of the receptor fluids were taken at predefined times over 6 hours and were analysed by UV–VIS high-performance liquid-chromatography. Histological examinations after methylene blue application were additionally performed to gather information about barrier disruption. Results Despite no visible pores in the stratum corneum, the microneedle pretreatment resulted in a twofold (200?μm) and threefold higher (300?μm) flux through the pretreated skin samples compared to untreated skin samples for ibuprofen and ketoprofen (LogKow-gt;-, melting point-lt;-00°C). The flux of the hydrophilic compounds diclofenac and paracetamol (logKow-lt;-, melting point-gt;-00°C) increased their amount by four (200?μm) to eight (300?μm), respectively. Conclusion Commercially available microneedle rollers with 200-00?μm long needles enhance the drug delivery of topically applied non-steroidal anti-inflammatory drugs and represent a valuable tool for percutaneous permeation enhancement particularly for substances with poor permeability due to a hydrophilic nature and high melting points.