Following-up skin penetration of lidocaine from different vehicles by Raman spectroscopic mapping

J Pharm Biomed Anal. 2018 May 30:154:1-6. doi: 10.1016/j.jpba.2018.02.056. Epub 2018 Mar 6.

Abstract

The application of local anesthetics, usually administered by subcutaneous injection, is common in the course of diagnostic, therapeutic, and cosmetic dermatology procedures. The effective dermal delivery of lidocaine could offer a solution to many adverse effects caused by needle insertion, such as pain, local reactions or toxicity, and additionally, it avoids the disruption of anatomical landmarks. Therefore, novel dermal formulations of local anesthetics are needed to overcome the barrier function of the skin and provide sufficient and prolonged anesthesia. In our study, we aimed to investigate and compare the penetration profiles of four different lidocaine containing formulations (hydrogel, oleogel, lyotropic liquid crystal and nanostructured lipid carrier) by Raman microscopic mapping of the drug. The application of Raman spectroscopy provided information about the spatial distribution of lidocaine in the skin ex vivo. The penetration of lidocaine from lyotropic liquid crystal and nanostructured carrier reached deeper skin layers and a higher amount of the drug was diffused into the skin, compared with hydrogel and oleogel. This study confirmed that nanostructured carriers can improve skin penetration properties of lidocaine and proved the applicability of Raman spectroscopy in the research of dermatological preparations ex vivo as a nondestructive, relatively easy and fast technique.

Keywords: Dermal delivery; Lidocaine; Lyotropic liquid crystal (LLC); Nanostructured lipid carrier (NLC); Raman spectroscopy; Skin penetration.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Cutaneous
  • Anesthetics, Local / administration & dosage*
  • Anesthetics, Local / pharmacokinetics
  • Chemistry, Pharmaceutical / methods
  • Drug Carriers / chemistry
  • Drug Carriers / pharmacokinetics*
  • Feasibility Studies
  • Female
  • Humans
  • Hydrogels / chemistry
  • Hydrogels / pharmacokinetics
  • Lidocaine / administration & dosage*
  • Lidocaine / pharmacokinetics
  • Lipids / chemistry
  • Lipids / pharmacokinetics
  • Nanoparticles / chemistry
  • Organic Chemicals / chemistry
  • Organic Chemicals / pharmacokinetics
  • Permeability
  • Skin / metabolism*
  • Skin Absorption / drug effects*
  • Spectrum Analysis, Raman

Substances

  • Anesthetics, Local
  • Drug Carriers
  • Hydrogels
  • Lipids
  • Organic Chemicals
  • oleogels
  • Lidocaine