Mucoadhesive multiparticulate patch for the intrabuccal controlled delivery of lidocaine

Eur J Pharm Biopharm. 2013 Apr;83(3):405-14. doi: 10.1016/j.ejpb.2012.10.004. Epub 2012 Nov 16.

Abstract

The aim of the present study was to prepare and evaluate patches for the controlled release of lidocaine in the oral cavity. Mucoadhesive buccal patches, containing 8 mg/cm(2) lidocaine base, were formulated and developed by solvent casting method technique, using a number of different bio-adhesive and film-forming semi-synthetic and synthetic polymers (Carbopol, Poloxamer, different type Methocel) and plasticizers (PEG 400, triethyl citrate); the patches were evaluated for bioadhesion, in vitro drug release and permeation using a modified Franz diffusion cell. A lidocaine/Compritol solid dispersion in the form of microspheres, embedded inside the patch, alone or together with free lidocaine, was also examined to prolong the drug release. The effects of the composition were evaluated considering a number of technological parameters and the release of the drug. All the formulations tested offer a variety of drug release mechanisms, obtaining a quick or delayed or prolonged anesthetic local activity with simple changes of the formulation parameters.

MeSH terms

  • Adhesives*
  • Anesthetics, Local / administration & dosage*
  • Anesthetics, Local / pharmacokinetics
  • Animals
  • Calorimetry, Differential Scanning
  • Cell Line
  • Lidocaine / administration & dosage*
  • Lidocaine / pharmacokinetics
  • Mice
  • Microscopy, Electron, Scanning
  • Mouth Mucosa*
  • Particle Size
  • Spectrum Analysis, Raman

Substances

  • Adhesives
  • Anesthetics, Local
  • Lidocaine