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Métodos Terapêuticos e Terapias MTCI
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1.
AAPS PharmSciTech ; 19(6): 2585-2597, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29916194

RESUMO

Amphotericin B (AmB), a potent antifungal drug, presents physicochemical characteristics that impair the development of suitable dosage forms. In order to overcome the AmB insolubility, several lipid carriers such as microemulsions have been developed. In this context, the bullfrog oil stands out as an eligible oily phase component, since its cholesterol composition may favor the AmB incorporation. Thus, the aim of this study was to develop a microemulsion based on bullfrog oil containing AmB. Moreover, its thermal stability, antifungal activity, and cytotoxicity in vitro were evaluated. The microemulsion formulation was produced using the pseudo-ternary phase diagram (PTPD) approach and the AmB was incorporated based on the pH variation technique. The antifungal activity was evaluated by determination of minimal inhibitory concentration (MIC) against different species of Candida spp. and Trichosporon asahii. The bullfrog oil microemulsion, stabilized with 16.8% of a surfactant blend, presented an average droplet size of 26.50 ± 0.14 nm and a polydispersity index of 0.167 ± 0.006. This system was able to entrap AmB up to 2 mg mL-1. The use of bullfrog oil as oily phase allowed an improvement of the thermal stability of the system. The MIC assay results revealed a growth inhibition for different strains of Candida spp. and were able to enhance the activity of AmB against T. asahii. The microemulsion was also able to reduce the AmB toxicity. Finally, the developed microemulsion showed to be a suitable system to incorporate AmB, improving the system's thermal stability, increasing the antifungal activity, and reducing the toxicity of this drug.


Assuntos
Anfotericina B/síntese química , Antifúngicos/síntese química , Portadores de Fármacos/síntese química , Emulsões/síntese química , Nanopartículas/química , Óleos/síntese química , Anfotericina B/administração & dosagem , Animais , Antifúngicos/administração & dosagem , Candida/efeitos dos fármacos , Candida/fisiologia , Portadores de Fármacos/administração & dosagem , Emulsões/administração & dosagem , Eritrócitos/efeitos dos fármacos , Eritrócitos/fisiologia , Humanos , Testes de Sensibilidade Microbiana/métodos , Nanopartículas/administração & dosagem , Óleos/administração & dosagem , Rana catesbeiana
2.
J Sci Food Agric ; 93(6): 1516-9, 2013 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22936615

RESUMO

BACKGROUND: Oil bodies isolated from sesame seeds coalesced to form large oil drops when they were solidified in a drying process commonly used for food products. The aim of this study was to develop a protocol to solidify oil bodies for long-term storage at room temperature. RESULTS: On the basis of testing several excipients, the coalescence of oil bodies could be effectively prevented when they were combined with mannitol. Sizes of oil bodies appeared similar under a light microscope before and after powderisation in combination with 70% or more mannitol. Artificial oil bodies were successfully generated with sesame oil, phospholipid and recombinant sesame caleosin. Following the developed protocol, native and artificial oil bodies were stably solidified in tablets. Both native and artificial oil bodies dissolved from the tablets remained stable after an accelerated stress test under a condition of 75% humidity at 40 °C for 4 months. CONCLUSION: A protocol was successfully developed for the solidification of native and artificial oil bodies in stable powder and tablet forms. This successful protocol is very likely to expedite the utilisation of artificial oil bodies in their potential applications.


Assuntos
Proteínas de Ligação ao Cálcio/química , Química Farmacêutica , Dessecação , Óleos/química , Fosfolipídeos/química , Proteínas de Plantas/química , Óleo de Gergelim/química , Sesamum/química , Estabilidade de Medicamentos , Armazenamento de Medicamentos , Manitol/química , Microscopia , Óleos/síntese química , Pós/química , Comprimidos/química , Temperatura
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