Design and evaluation of lidocaine- and prilocaine-coloaded nanoparticulate drug delivery systems for topical anesthetic analgesic therapy: a comparison between solid lipid nanoparticles and nanostructured lipid carriers

Drug Des Devel Ther. 2017 Sep 18:11:2743-2752. doi: 10.2147/DDDT.S141031. eCollection 2017.

Abstract

Purpose: Topical anesthesia analgesic therapy has diverse applicability in solving the barrier properties of skin and unfavorable physicochemical properties of drugs. Lidocaine (LID) combined with prilocaine (PRI) has been used as a topical preparation for dermal anesthesia for treatment of conditions such as paresthesia.

Materials and methods: In this study, for combination anesthesia and overcoming the drawbacks of LID and PRI, respectively, LID- and PRI-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were prepared and characterized by determination of their particle size, drug loading capacity, stability, in vitro drug release behavior and in vitro cellular viability. Ex vivo skin permeation and in vivo anesthesia analgesic efficiency of these two systems were also evaluated and compared.

Results: Results revealed that combination delivery of the dual drugs exhibited more remarkable efficiency than signal drug-loaded systems. SLN systems have better ex vivo skin permeation ability than NLCs. NLC systems revealed a stronger in vivo anesthesia analgesic effect than SLN systems.

Conclusion: It can be concluded that SLNs and NLCs have different advantages, and that both carriers are promising dual drug delivery systems for topical anesthetic analgesic therapy.

Keywords: lidocaine; nanostructured lipid carriers; prilocaine; solid lipid nanoparticles; topical anesthesia.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Cutaneous
  • Anesthetics, Local / administration & dosage*
  • Anesthetics, Local / pharmacokinetics
  • Anesthetics, Local / pharmacology
  • Animals
  • BALB 3T3 Cells
  • Chemistry, Pharmaceutical / methods
  • Drug Carriers / chemistry
  • Drug Delivery Systems*
  • Drug Liberation
  • Lidocaine / administration & dosage*
  • Lidocaine / pharmacokinetics
  • Lidocaine / pharmacology
  • Lipids / chemistry
  • Mice
  • Nanoparticles
  • Particle Size
  • Prilocaine / administration & dosage*
  • Prilocaine / pharmacokinetics
  • Prilocaine / pharmacology
  • Rats
  • Rats, Wistar
  • Skin / metabolism
  • Skin Absorption

Substances

  • Anesthetics, Local
  • Drug Carriers
  • Lipids
  • Prilocaine
  • Lidocaine