Avaliação do aumento da solubilidade aquosa do praziquantel incorporado em microesferas de poli(3-hidroxibutirato) e Eudragit®



Título del documento: Avaliação do aumento da solubilidade aquosa do praziquantel incorporado em microesferas de poli(3-hidroxibutirato) e Eudragit®
Revue: Acta scientiarum. Health science
Base de datos: PERIÓDICA
Número de sistema: 000366075
ISSN: 1679-9291
Autores: 1
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Instituciones: 1Universidade da Regiao de Joinville, Departamento de Farmacia, Joinville, Santa Catarina. Brasil
Año:
Periodo: Ene-Jun
Volumen: 35
Número: 1
Paginación: 91-96
País: Brasil
Idioma: Portugués
Tipo de documento: Artículo
Enfoque: Analítico, descriptivo
Resumen en inglés Praziquantel is the drug of choice for the treatment of schistosomiasis, however, its low water solubility may undermine the oral bioavailability. In this study, praziquantel was incorporated into microspheres prepared with poly(3-hydroxybutyrate) (PHB) and a polymethacrylate (Eudragit® E), using an emulsion-solvent evaporation method, in order to improve its aqueous solubility. Microparticles prepared with PHB had spherical shape and encapsulation efficiency of 78%. When prepared with Eudragit® E/PHB at a ratio of 50/50 the microspheres were porous and encapsulated 42% of the drug, and for a ratio of 75/25 the microspheres were more porous than those of the previous formulations, with an encapsulation efficiency of 52%. Dissolution in vitro led to a significant improvement in the aqueous solubility of praziquantel incorporated into Eudragit® E/PHB 75/25 microspheres. This increased solubility is linked to the high porosity of the microspheres and the use of Eudragit® E as a hydrophilic carrier
Resumen en portugués Praziquantel is the drug of choice for the treatment of schistosomiasis, however, its low water solubility may undermine the oral bioavailability. In this study, praziquantel was incorporated into microspheres prepared with poly(3-hydroxybutyrate) (PHB) and a polymethacrylate (Eudragit® E), using an emulsion-solvent evaporation method, in order to improve its aqueous solubility. Microparticles prepared with PHB had spherical shape and encapsulation efficiency of 78%. When prepared with Eudragit® E/PHB at a ratio of 50/50 the microspheres were porous and encapsulated 42% of the drug, and for a ratio of 75/25 the microspheres were more porous than those of the previous formulations, with an encapsulation efficiency of 52%. Dissolution in vitro led to a significant improvement in the aqueous solubility of praziquantel incorporated into Eudragit® E/PHB 75/25 microspheres. This increased solubility is linked to the high porosity of the microspheres and the use of Eudragit® E as a hydrophilic carrier
Disciplinas: Medicina,
Química
Palabras clave: Química farmacéutica,
Parasitología,
Antiparasitarios,
Praziquantel,
Microencapsulación,
Solubilidad,
Poli(3-hidroxibutirato),
Eudragit
Keyword: Medicine,
Chemistry,
Medicinal chemistry,
Parasitology,
Antiparasitic agents,
Praziquantel,
Microencapsulation,
Solubility,
Poly(3-hydroxybutyrate),
Eudragit
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