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Int J Pharm ; 483(1-2): 188-99, 2015 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-25681721

RESUMO

An essential in vivo drug delivery system of a momordica anti-HIV protein, MAP30, was developed through encapsulating in chemically synthesized matrices of zirconium egg- and soy-phosphatidylcholines, abbreviated to Zr/EPC and Zr/SPC, respectively. Matrices were characterized by transmission electron microscopy and powder X-ray diffractometry studies. Zr/EPC granule at an approximate diameter of 69.43±7.78 nm was a less efficient encapsulator than the granule of Zr/SPC. Interlayer spacing of the matrices encapsulating MAP30 increased from 8.8 and 9.7 Å to 7.4 and 7.9 nm, respectively. In vivo kinetics on degradation and protein release was performed by analyzing the serum sampling of intravenously injected SPF chickens. The first order and biphasic variations were obtained for in vivo kinetics using equilibrium dialysis. Antimicrobial and anti-HIV assays yielded greatly decreased MIC50 and EC50 values of nanoformulated MAP30. An acute toxicity of MAP30 encapsulated in Zr/EPC occurred at a single intravenous dose above 14.24 mg/kg bw in NIH/KM/ICR mice. The folding of MAP30 from Zr/EPC sustained in vivo chickens for more than 8 days in high performance liquid chromatography assays. These matrices could protect MAP30 efficiently with strong structure retention, lowered toxicity and prolonged in vivo life.


Assuntos
Antibacterianos/farmacologia , Fármacos Anti-HIV/farmacologia , Bactérias/efeitos dos fármacos , Sistemas de Liberação de Medicamentos , HIV-1/efeitos dos fármacos , Nanocápsulas/química , Fosfatidilcolinas/química , Proteínas Inativadoras de Ribossomos Tipo 2/metabolismo , Zircônio/química , Animais , Antibacterianos/química , Antibacterianos/metabolismo , Fármacos Anti-HIV/química , Fármacos Anti-HIV/metabolismo , Injeções Intravenosas , Camundongos , Camundongos Endogâmicos , Estrutura Molecular , Nanocápsulas/administração & dosagem , Tamanho da Partícula , Fosfatidilcolinas/administração & dosagem , Proteínas Inativadoras de Ribossomos Tipo 2/administração & dosagem , Proteínas Inativadoras de Ribossomos Tipo 2/química , Propriedades de Superfície , Zircônio/administração & dosagem
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