0109 : Increase liposomes cardioprotective activity of pyridostigmine - 05/05/15
Résumé |
Pyridostigmine (PIR), a reversible anticholinestesic, has its cardioprotective effects demonstrated by the reduction of the QT interval of the eletrocardiogram ECG in patients with heart deases. Experimentally this QT prolongation is induced by adrenergic stimulation. However, its short half-life and the incidence of side effects are factors that limit its prolonged use. This study was aimed to investigate the cardioprotective activity of pyridostigmine conveyed in convetional multilamelar liposomes administered subcutaneously. Two multilamellar liposomal formulations were developed and tested: one consisting of dioleil phosphatidylcholine (DOPC) and cholesterol (CHOL) and the other consisting of diasteroylphosphatidylcholine (DSPC) and CHOL. The encapsulation efficiency determined was 15,4% and 23,4% respectively. The cardioprotective activity of PIR was evaluated in rats for its ability to prevent cardiovascular disorders, demonstrated, in signs of blood pressure (BP) and ECG induced by IV administration of noradrenaline (NA). After administration of 10mg/kg NA, the DSPC and DOPC liposomal formulations containing PIR were able to reduce significantly the QT interval, with a maximum inhibition of 76.4% and 73.0% respectively. Both formulations DSPC: CHOL and DOPC: CHOL, attenuated the increase in BP within 12 to 24 hours respectively. As the QT prolongation is a predictior of sudden death and the PIR was able to prevent its prolongation after sympathetic stimulation, it could be suggested that PIR in liposomes administered sbcutaneously has cardioprotective activity.
Le texte complet de cet article est disponible en PDF.Vol 7 - N° 2
P. 149 - avril 2015 Retour au numéroBienvenue sur EM-consulte, la référence des professionnels de santé.
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