Abstract
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.
Highlights
Praziquantel is the drug of choice for the treatment of schistosomiasis, its low water solubility may undermine the oral bioavailability
A esquistossomose é uma doença que afeta milhares de pessoas no Brasil e no mundo, enquadrada no grupo das denominadas doenças negligenciadas, as quais recebem pouco investimento financeiro em pesquisa e desenvolvimento de novos medicamentos (KATZ; PEIXOTO, 2000)
A presença de poros de grande diâmetro na superfície das microesferas, conforme se observou na Figura 1, pode ter contribuído para favorecer a dissolução do praziquantel por possibilitar a entrada do meio de dissolução no interior da matriz polimérica, facilitando a solubilização do fármaco
Summary
O praziquantel foi adquirido da Attivos Magisttrais (São Paulo, Estado de São Paulo). O poli(3-hidroxibutirato) foi gentilmente cedido pela PHB Industrial (Serrana, Estado de São Paulo) e o Eudragit® E pela Almapal S.A. (Biotec) e poli(álcool vinílico) adquirido da Vetec Química (Rio de Janeiro, Estado do Rio de Janeiro) Diclorometano e ácido clorídrico p.a. (Biotec) e poli(álcool vinílico) adquirido da Vetec Química (Rio de Janeiro, Estado do Rio de Janeiro)
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