Enhanced ex vivo buccal transport of propranolol: evaluation of phospholipids as permeation enhancers

Arch Pharm Res. 2003 May;26(5):421-5. doi: 10.1007/BF02976701.

Abstract

The aim of the present study was to evaluate the effects of two phospholipid permeation enhancers, lysophosphatidylcholine (LPC) and didecanoylphosphatidylcholine (DDPC), along with a fusidic acid derivative, sodium taurodihydrofusidate (STDHF) and ethanol (EtOH) on the buccal transport of propranolol hydrochloride (PPL) using an ex vivo buccal diffusion model. The permeation rate of [3H]PPL as measured by steady-state fluxes increased with increasing EtOH concentration. A significant flux enhancement (P<0.05) was achieved by EtOH at 20 and 30 %v/v concentrations. At a 0.5 %w/v permeation enhancer concentration, the buccal permeation of [3H]PPL was significantly enhanced by all the enhancers studied (i.e., LPC, DDPC and STDHF) compared to the control (phosphate-buffered saline pH 7.4, PBS). LPC and DDPC displayed a greater degree of permeation enhancement compared with STDHF and EtOH-PBS mixtures with an enhancement ratio of 3.2 and 2.9 for LPC and DDPC, respectively compared with 2.0 and 1.5 for STDHF and EtOH:PBS 30:70 %v/v mixture, respectively. There was no significant difference between LPC and DDPC for the flux values and apparent permeability coefficients of [3H]PPL. These results suggest that phospholipids are suitable as permeation enhancers for the buccal delivery of drugs.

MeSH terms

  • Absorption
  • Administration, Buccal
  • Animals
  • Drug Synergism
  • Ethanol / pharmacology
  • Fusidic Acid / analogs & derivatives
  • Fusidic Acid / pharmacology
  • In Vitro Techniques
  • Lysophosphatidylcholines / pharmacology*
  • Mouth Mucosa / drug effects
  • Mouth Mucosa / metabolism*
  • Permeability
  • Phosphatidylcholines / pharmacology*
  • Propranolol / pharmacokinetics*
  • Swine

Substances

  • Lysophosphatidylcholines
  • Phosphatidylcholines
  • didecanoylphosphatidylcholine
  • Ethanol
  • Fusidic Acid
  • Propranolol