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1.
ACS Infect Dis ; 9(3): 423-449, 2023 03 10.
Artigo em Inglês | MEDLINE | ID: mdl-36795604

RESUMO

Leishmaniasis is an infectious disease responsible for a huge rate of morbidity and mortality in humans. Chemotherapy consists of the use of pentavalent antimonial, amphotericin B, pentamidine, miltefosine, and paromomycin. However, these drugs are associated with some drawbacks such as high toxicity, administration by parenteral route, and most seriously the resistance of some strains of the parasite to them. Several strategies have been used to increase the therapeutic index and reduce the toxic effects of these drugs. Among them, the use of nanosystems that have great potential as a site-specific drug delivery system stands out. This review aims to compile results from studies that were carried out using first- and second-line antileishmanial drug-carrying nanosystems. The articles referred to here were published between 2011 and 2021. This study shows the promise of effective applicability of drug-carrying nanosystems in the field of antileishmanial therapeutics, with the perspective of providing better patient adherence to treatment, increased therapeutic efficacy, reduced toxicity of conventional drugs, as well as the potential to efficiently improve the treatment of leishmaniasis.


Assuntos
Antiprotozoários , Leishmaniose , Humanos , Preparações Farmacêuticas , Antiprotozoários/farmacologia , Antiprotozoários/uso terapêutico , Leishmaniose/tratamento farmacológico , Pentamidina/farmacologia , Pentamidina/uso terapêutico , Paromomicina/farmacologia
2.
J Nat Prod ; 82(12): 3208-3220, 2019 12 27.
Artigo em Inglês | MEDLINE | ID: mdl-31815454

RESUMO

The physicochemical characteristics of nanostructured suspensions are important prerequisites for the success of new drug development. This work aimed to develop nanometric systems containing Cymbopogon densiflorus leaf essential oil and to evaluate their antimicrobial activity. The essential oil was isolated by hydrodistillation from leaves and analyzed by GC-MS. The main constituents were found to be trans-p-mentha-2,8-dien-1-ol, cis-p-mentha-2,8-dien-1-ol, trans-p-mentha-1(7),8-dien-2-ol, cis-piperitol, and cis-p-mentha-1(7),8-dien-2-ol. In silico prediction analysis suggested that this oil possesses antimicrobial potential and the main mechanism of action might be the peptidoglycan glycosyltransferase inhibition. Nanoemulsions were prepared by the phase inversion method, and liposomes were made by the film hydration method. Qualitative evaluation of the antimicrobial activity was performed by the diffusion disk assay with 24 microorganisms; all of them were found to be sensitive to the essential oil. Subsequently, this property was quantified by the serial microdilution technique, where the nanoformulations demonstrated improved activity in comparison with the free oil. Bactericidal action was tested by the propidium iodide method, which revealed that free essential oil and nanoemulsion increased cytoplasmic membrane permeability, while no difference was observed between negative control and liposome. These results were confirmed by images obtained using transmission electron microscopy. This study has shown an optimization in the antimicrobial activity of C. densiflorus essential oil by a nanoemulsion and a liposomal formulation of the active substances.


Assuntos
Anti-Infecciosos/farmacologia , Cymbopogon/química , Nanoestruturas , Óleos Voláteis/farmacologia , Folhas de Planta/química , Animais , Anti-Infecciosos/química , Bactérias/efeitos dos fármacos , Linhagem Celular , Permeabilidade da Membrana Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Fungos/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Concentração de Íons de Hidrogênio , Camundongos , Testes de Sensibilidade Microbiana , Microscopia Eletrônica de Transmissão , Óleos Voláteis/química , Tamanho da Partícula , Relação Quantitativa Estrutura-Atividade
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