Transcutaneous anaesthetic nano-enabled hydrogels for eyelid surgery

Int J Pharm. 2020 Mar 15:577:119003. doi: 10.1016/j.ijpharm.2019.119003. Epub 2020 Jan 11.

Abstract

Local anaesthetics are administered as a diffuse superficial slow injection in blepharoplasty. Current transcutaneous local anaesthetic formulations are not licensed for use on the face due to safety concerns. Here we report for the first time the permeation of local anaesthetics (lidocaine, bupivacaine loaded SNEDDS and their hydrogels) across human eyelid and mouse skin as a novel and ocular safe formulation for eyelid surgery. SNEDDS were loaded with high levels of anaesthetics and incorporated within carbomer hydrogels to yield nano-enabled gels. Lidocaine hydrogels have a significantly reduced lag time compared to EMLA, while they enhance lidocaine flux across human eyelid skin by 5.2 fold. Ex vivo tape stripping experiments indicated localisation of anaesthetics within the stratum corneum and dermis. Initial histopathological studies have shown no apparent signs of skin irritation. These results highlight the potential clinical capability of nano-enabled anaesthetic hydrogels as a non-invasive anaesthetic procedure for eyelid surgery.

Keywords: Anaesthetics; Bupivacaine; Eyelid; Franz cell diffusion assays; Hydrogels; Lidocaine; Self-nanoemulsifying drug delivery systems (SNEDDS); Tape stripping.

MeSH terms

  • Acrylic Resins / chemistry
  • Administration, Cutaneous
  • Anesthetics, Local / adverse effects
  • Anesthetics, Local / chemistry
  • Anesthetics, Local / pharmacology
  • Animals
  • Bupivacaine / administration & dosage
  • Bupivacaine / chemistry*
  • Drug Delivery Systems
  • Emulsions / chemistry*
  • Emulsions / pharmacology
  • Eyelids / surgery*
  • Humans
  • Hydrogels / chemistry*
  • Lidocaine / administration & dosage
  • Lidocaine / adverse effects
  • Lidocaine / chemistry*
  • Lidocaine / pharmacology
  • Lidocaine, Prilocaine Drug Combination / pharmacology
  • Male
  • Mice
  • Nanogels / chemistry*
  • Nanotechnology / methods
  • Ophthalmologic Surgical Procedures / methods*
  • Skin Absorption / drug effects

Substances

  • Acrylic Resins
  • Anesthetics, Local
  • Emulsions
  • Hydrogels
  • Lidocaine, Prilocaine Drug Combination
  • Nanogels
  • carbomer
  • Lidocaine
  • Bupivacaine