DEFAR - Departamento de Farmácia

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Reduced cardiovascular alterations of tartar emetic administered in long-circulating liposomes in rats.
(2010) Maciel, Naira Rezende; Reis, Priscila Gomes dos; Kato, Kelly Cristina; Vidal, Alessandra Teixeira; Guimarães, Homero Nogueira; Frezard, Frederic Jean Georges; Barcellos, Neila Marcia Silva; Guimarães, Andrea Grabe
Trivalent antimonial drugs, including tartar emetic (TA), are known to induce important cardiotoxicity observed by electrocardiographic abnormalities. Liposome encapsulation was found to reduce the overall acute toxicity of TA. The present work investigated the cardiovascular parameters alterations of rats submitted to the treatment with free and encapsulated TA in long-circulating liposomes. Liposomes were made using lipids DSPC, DSPE-PEG and cholesterol. The cardiovascular signals, electrocardiogram (ECG) and arterial blood pressure (AP), were recorded from anaesthetized Wistar rats after intravenous (IV) administration of a single specially high dose (17 mg/kg) of TA in liposomes and in free form. The IV administration of TA solution caused significant increase of QT interval of ECG and significant reduction of AP when compared to the control group. These alterations were not observed when liposomes TA were administered and the profile of ECG and AP data was quite similar to the control groups. In conclusion, a liposomal formulation of TA showed a reduced cardiotoxic profile for TA when compared to the free form.