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1.
Parasitology ; 145(8): 1075-1083, 2018 07.
Artigo em Inglês | MEDLINE | ID: mdl-29223181

RESUMO

Artemether (ATM) cardiotoxicity, its short half-life and low oral bioavailability are the major limiting factors for its use to treat malaria. The purposes of this work were to study free-ATM and ATM-loaded poly-ε-caprolactone nanocapules (ATM-NC) cardiotoxicity and oral efficacy on Plasmodium berghei-infected mice. ATM-NC was obtained by interfacial polymer deposition and ATM was associated with polymeric NC oily core. For cardiotoxicity evaluation, male black C57BL6 uninfected or P. berghei-infected mice received, by oral route twice daily/4 days, vehicle (sorbitol/carboxymethylcellulose), blank-NC, free-ATM or ATM-NC at doses 40, 80 or 120 mg kg-1. Electrocardiogram (ECG) lead II signal was obtained before and after treatment. For ATM efficacy evaluation, female P. berghei-infected mice were treated the same way. ATM-NC improved antimalarial in vivo efficacy and reduced mice mortality. Free-ATM induced significantly QT and QTc intervals prolongation. ATM-NC (120 mg kg-1) given to uninfected mice reduced QT and QTc intervals prolongation 34 and 30%, respectively, compared with free-ATM. ATM-NC given to infected mice also reduced QT and QTc intervals prolongation, 28 and 27%, respectively. For the first time, the study showed a nanocarrier reducing cardiotoxicity of ATM given by oral route and it was more effective against P. berghei than free-ATM as monotherapy.


Assuntos
Antimaláricos/administração & dosagem , Artemeter/administração & dosagem , Cardiotoxicidade/prevenção & controle , Nanocápsulas/química , Plasmodium berghei/efeitos dos fármacos , Administração Oral , Animais , Antimaláricos/toxicidade , Artemeter/toxicidade , Modelos Animais de Doenças , Eletrocardiografia , Feminino , Malária/tratamento farmacológico , Masculino , Camundongos , Camundongos Endogâmicos C57BL
2.
Pharm Dev Technol ; 19(4): 454-9, 2014 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-23682846

RESUMO

Pyridostigmine has cardioprotective activity in both free and liposomal forms. This study aimed to develop and characterize liposomal formulations of pyridostigmine. For this, a spectrophotometric ultraviolet (UV) analytical method, at 270 nm, was developed and validated to quantify liposomal pyridostigmine. The method was linear in ranges from 0.02 to 0.09 mg/mL. The accuracy of this method was determined intra- and inter-day; the results of coefficient of variation were of 1.73-2.72% and 0.32-2.32%, respectively. The accuracy ranged between 99.45% and 101.12%. The method has not changed by influence of liposomal matrix and demonstrated being able to quantify pyridostigmine in liposomes. Two liposomal multilamellar formulations were developed: a constituted by dystearoyl-phosphatidylcholine (DSPC) and cholesterol (CHOL) other by dioleil-phosphatidylcholine (DOPC) and CHOL. The encapsulation efficiency was determined as 23.4% and 15.4%, respectively. Analyses of size and release of pyridostigmine from the formulations were made and the results showed that the formulations are viable for future studies in vivo.


Assuntos
Lipossomos/química , Brometo de Piridostigmina/química , Química Farmacêutica/métodos , Colesterol/química , Portadores de Fármacos/química , Tamanho da Partícula , Fosfatidilcolinas/química
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