The in vitro passive diffusion of S-ibuprofen (S-IB) and RS-ibuprofen (RS-IB) through human epidermis was determined to study the effects of drug chirality. S-IB has a lower melting point (Tm =54◦C) than RS-IB (Tm =77◦C) and, therefore, a greater solubility (S-IB: 127±1_g/mL; RS-IB: 81±1_g/mL). Supersaturated plasters were prepared by using a poly(dimethylsiloxane) adhesive and Eugragit® RL and propylene glycol as antinucleant agents. The in vitro skin permeation profiles were determined by Franz cells and human epidermis obtained from three different donors. The permeation profiles of S-IB from saturated solutionsresulted statistically higher than those of RS-IB (p < 0.002). When plasters were used, no differences were noticeable between the enantiomer and racemate (p > 0.17). The latter unexpected results could be explained considering that the RS-IB or S-IB in vitro release rate constants, determined using 3% w/w or 6% w/w loaded plasters, were not statistically different, suggesting that the drug diffusivity within the adhesive matrix represented the rate limiting step to the skin absorption.
Effect of drug chirality on the skin permeability of ibuprofen / F. Cilurzo, E. Alberti, P. Minghetti, C.G.M. Gennari, A. Casiraghi, L. Montanari. - In: INTERNATIONAL JOURNAL OF PHARMACEUTICS. - ISSN 0378-5173. - 386:1-2(2010 Feb), pp. 71-76.
|Titolo:||Effect of drug chirality on the skin permeability of ibuprofen|
CILURZO, FRANCESCO (Primo)
ALBERTI, ELISABETTA (Secondo)
CASIRAGHI, ANTONELLA (Penultimo)
MONTANARI, LUISA (Ultimo)
|Settore Scientifico Disciplinare:||Settore CHIM/09 - Farmaceutico Tecnologico Applicativo|
|Data di pubblicazione:||feb-2010|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1016/j.ijpharm.2009.10.053|
|Appare nelle tipologie:||01 - Articolo su periodico|