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Mechanism of action of Azone as a percutaneous penetration enhancer: Lipid bilayer fluidity and transition temperature effects

Beastall, JC; Hadgraft, J; Washington, C; (1988) Mechanism of action of Azone as a percutaneous penetration enhancer: Lipid bilayer fluidity and transition temperature effects. International Journal of Pharmaceutics , 43 (3) pp. 207-213. 10.1016/0378-5173(88)90275-X.

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Abstract

Azone is an effective penetration enhancer for the percutaneous delivery ofcertain topically applied drugs. Fundamental physicochemical experiments have been performed to elucidate the mechanism of action of Azone. The penetration enhancing effect of Azone is believed to be due to its increasing the fluidity of the intercellular lipid bilayers of the stratum corneum. Phospholipid vesicles were chosen as a simple model to represent these bilayers. The effect of Azone on phase transition temperature and lipid fluidity was studied using turbidity and fluorescent probe (pyrene excimer) technique. Addition of increasing amounts of Azone to the bilayer resulted in lowering of phase transition temperature, shown by turbidity of vesicle suspensions, and an increase in lipid fluidity, shown by changes in pyrene fluorescence. The results suggest that Azone would interact with striatum corneum lipids in a similar manner, thereby reducing the diffusional resistance of the stratum corneum to drugs with balanced hydrophilic-lipophilic characteristics. © 1988.

Type: Article
Title: Mechanism of action of Azone as a percutaneous penetration enhancer: Lipid bilayer fluidity and transition temperature effects
DOI: 10.1016/0378-5173(88)90275-X
UCL classification: UCL > School of Life and Medical Sciences
UCL > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
URI: http://discovery.ucl.ac.uk/id/eprint/1435213
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