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Titolo:
A CALORIMETRIC STUDY ON THE IDEBENONE-PHOSPHOLIPID MEMBRANE INTERACTION
Autore:
FRESTA M; VENTURA CA; MEZZASALMA E; PUGLISI G;
Indirizzi:
UNIV CATANIA,DIPARTIMENTO SCI FARMACEUT,VIALE ANDREA DORIA 6 I-95125 CATANIA ITALY UNIV CATANIA,DIPARTIMENTO SCI FARMACEUT I-95125 CATANIA ITALY
Titolo Testata:
International journal of pharmaceutics
fascicolo: 1-2, volume: 163, anno: 1998,
pagine: 133 - 143
SICI:
0378-5173(1998)163:1-2<133:ACSOTI>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
CEREBRAL POSTISCHEMIC REPERFUSION; MODIFIED BETA-CYCLODEXTRINS; CDP-CHOLINE; CYTIDINE-5'-DIPHOSPHATE CHOLINE; LIPID-PEROXIDATION; BRAIN MITOCHONDRIA; MODEL; RATS; LIPOSOMES; ISCHEMIA;
Keywords:
IDEBENONE; MEMBRANE; LIPOSOME; DIFFERENTIAL SCANNING CALORIMETRY; IN VITRO INTERACTION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
29
Recensione:
Indirizzi per estratti:
Citazione:
M. Fresta et al., "A CALORIMETRIC STUDY ON THE IDEBENONE-PHOSPHOLIPID MEMBRANE INTERACTION", International journal of pharmaceutics, 163(1-2), 1998, pp. 133-143

Abstract

Idebenone is a drug acting at the level of the central nervous systemand is largely employed in the treatment of various cerebral diseases. To evaluate in vitro the possible in vivo interaction with biological membranes and to carry out a pre-formulation study for the realization of an idebenone-loaded liposome system, the interaction between this drug and model membranes made up of various naturally occurring phospholipids was investigated. The idebenone-membrane interaction was studied by differential scanning calorimetry (DSC). The presence of the drug noticeably influenced the thermotropic behavior of the membranes, shifting the main transition peak temperature towards lower values andbroadening the peak. The extent of the perturbation of the membrane properties is a function of the content of idebenone. In particular, beyond an idebenone molar fraction of 0.09 a phase segregation of the lipid components constituting the bilayers was detected. These features showed that the drug is fully inserted into the bilayer matrix of the various membranes. The idebenone-membrane interaction is enhanced by the presence of negatively charged phospholipids. A kinetic experiment showed that the limiting step in the interaction with a biological substrate could be the diffusion process through the aqueous compartmentsrather than the interaction with the biological membrane bilayers. The formulation of a liposomal drug delivery system containing idebenonemay improve the pharmaceutical and therapeutic properties of the drug. (C) 1998 Elsevier Science B.V. All rights reserved.

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Documento generato il 08/07/20 alle ore 00:51:18