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Enhanced Ex Vivo Buccal Transport of Propranolol: Evaluation of Phospholipids as Permeation Enhancers  

Lee, Jae-Hwi (Department of Industrial and Physical Pharmacy, School of Pharmacy, Purdue University)
Choi, Young-Wook (College of Pharmacy, Chung-Ang University)
Publication Information
Archives of Pharmacal Research / v.26, no.5, 2003 , pp. 421-425 More about this Journal
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 [$^3 H$]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 [$^3 H$]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 [$^3$H]PPL. These results suggest that phospholipids are suitable as permeation enhancers for the buccal delivery of drugs.
Keywords
Buccal delivery; Propranolol; Permeation enhancer; Lysophosphatidylcholine; Didecanoylphosphatidylcholine; Sodium taurodihydrofusidate;
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