The effects of different concentrations of beta -cyclodextrin (beta -Cyd), hydroxypropyl-beta -cyclodextrin (HP-beta -CyD) and 2,6-di-O-methyl-beta -cyclodextrin (DM-beta -CyD) on percutaneous absorption of papaverine hydrochloride (PAY) were investigated. Abdominal rat skin mounted in Franz cells was used for in vitro experiments. To evaluate CyD interaction with a bilayer structure model, dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and DPPC-Chol (8:2 mole ratio) vesicles were used. CyD vesicle interaction was evaluated by differential scanning calorimetry. Permeation through rat skin and calorimetric experiments demonstrated that at low concentrations DM-beta -CyD shows higher enhancer activity as a possible result of a perturbing action on the skin by a complexation of its lipid components, but at higher concentrations HP-beta -CyD is the most effective. By considering that HP-beta -CyD presents a very moderate destabilizing action on the skin, we conclude that a 10% aqueous solution of this macrocycle appears to be the most suitable transdermal absorption enhancer for PAP.

Biomembrane model interaction and percutaneous absorption of papaverine through rat skin: Effects of cyclodextrins as penetration enhancers

Paolino D;FRESTA M
2001-01-01

Abstract

The effects of different concentrations of beta -cyclodextrin (beta -Cyd), hydroxypropyl-beta -cyclodextrin (HP-beta -CyD) and 2,6-di-O-methyl-beta -cyclodextrin (DM-beta -CyD) on percutaneous absorption of papaverine hydrochloride (PAY) were investigated. Abdominal rat skin mounted in Franz cells was used for in vitro experiments. To evaluate CyD interaction with a bilayer structure model, dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and DPPC-Chol (8:2 mole ratio) vesicles were used. CyD vesicle interaction was evaluated by differential scanning calorimetry. Permeation through rat skin and calorimetric experiments demonstrated that at low concentrations DM-beta -CyD shows higher enhancer activity as a possible result of a perturbing action on the skin by a complexation of its lipid components, but at higher concentrations HP-beta -CyD is the most effective. By considering that HP-beta -CyD presents a very moderate destabilizing action on the skin, we conclude that a 10% aqueous solution of this macrocycle appears to be the most suitable transdermal absorption enhancer for PAP.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.12317/8713
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