International Journal of Pharmaceutics 2014-07-20

DSC investigation of the effect of the new sigma ligand PPCC on DMPC lipid membrane.

Maria Grazia Sarpietro, Maria Lorena Accolla, Annamaria Cova, Orazio Prezzavento, Francesco Castelli, Simone Ronsisvalle

Index: Int. J. Pharm. 469(1) , 88-93, (2014)

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Abstract

The new sigma ligand cis-(±)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl) methyl]-1-(4-methylphenyl) cyclopropanecarboxylate [(±)-PPCC] is a promising tool for the treatment of various diseases. With the aim to investigate the absorption of (±)-PPCC by the cell membranes, in this study we evaluated the influence on thermotropic behavior of membrane model exerted by PPCC both as free base or as oxalic salt. To fulfill this purpose differential scanning calorimetry was used. The findings highlight that PPCC affects the thermodynamic parameters of phospholipids in different manner depending on whether it is in the salt or base form as well as function of the amount of drugs dispersed in the lipid matrix. The salt form of PPCC was uptaken by the membrane model faster than the free base. In addition, preliminary information on the use of a lipophilic carrier for PPCC was obtained.Copyright © 2014 Elsevier B.V. All rights reserved.