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Enhancedex vivo buccal transport of propranolol: Evaluation of phospholipids as permeation enhancers

Archives of Pharmacal Research volume 26, Article number: 421 (2003) Cite this article

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 anex 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.

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Authors and Affiliations

  1. Department of Industrial and Physical Pharmacy, School of Pharmacy, Purdue University, 47907-2091, West Lafayette, IN, USA

    Jaehwi Lee

  2. College of Pharmacy, Chung-Ang University, 156-756, Seoul, Korea

    Young Wook Choi

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  1. Jaehwi Lee
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  2. Young Wook Choi
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Correspondence to Jaehwi Lee.

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Lee, J., Choi, Y.W. Enhancedex vivo buccal transport of propranolol: Evaluation of phospholipids as permeation enhancers. Arch Pharm Res 26, 421 (2003). https://doi.org/10.1007/BF02976701

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  • DOI: https://doi.org/10.1007/BF02976701

Key words

  • Buccal delivery
  • Propranolol
  • Permeation enhancer
  • Lysophosphatidylcholine
  • Didecanoylphosphatidylcholine
  • Sodium taurodihydrofusidate