title: (-)-Hinokinin-loaded poly(D,-lactide-co-glycolide) microparticles for Chagas disease.
abstract: The (-)-hinokinin display high activity against Trypanosoma cruzi in vitro and in vivo. (-)-Hinokinin-loaded poly(D,L-lactide-co-glycolide) microparticles were prepared and characterized in order to protect (-)-hinokinin of biological interactions and promote its sustained release for treatment of Chagas disease. The microparticles contain (-)-hinokinin were prepared by the classical method of the emulsion/solvent evaporation. The scanning electron microscopy, light-scattering analyzer were used to study the morphology and particle size, respectively. The encapsulation efficiency was determined, drug release studies were kinetically evaluated, and the trypanocidal effect was evaluated in vivo. (-)-Hinokinin-loaded microparticles obtained showed a mean diameter of 0.862 microm with smooth surface and spherical shape. The encapsulation efficiency was 72.46 +/- 2.92% and developed system maintained drug release with Higuchi kinetics. The preparation method showed to be suitable, since the morphological characteristics, encapsulation efficiency, and in vitro release profile were satisfactory. In vivo assays showed significant reduction of mice parasitaemia after administration of (-)-hinokinin-loaded microparticles. Thus, the developed microparticles seem to be a promising system for sustained release of (-)-hinokinin for treatment of Chagas disease.
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, Avenida do Café s/n, 14040-903 Ribeirão Preto, SP, Brazil.
authors.forename: Juliana
authors.initials: J
authors.lastname: Saraiva
authors.forename: Ana Amélia Moreira
authors.initials: AA
authors.lastname: Lira
authors.forename: Viviane Rodrigues
authors.initials: VR
authors.lastname: Esperandim
authors.forename: Daniele
authors.initials: D
authors.lastname: da Silva Ferreira
authors.forename: Antônio Sérgio
authors.initials: AS
authors.lastname: Ferraudo
authors.forename: Jairo Kenupp
authors.initials: JK
authors.lastname: Bastos
authors.forename: Márcio Luís Andrade
authors.initials: ML
authors.lastname: E Silva
authors.forename: Cristiane Masetto
authors.initials: CM
authors.lastname: de Gaitani
authors.forename: Sérgio
authors.initials: S
authors.lastname: de Albuquerque
authors.forename: Juliana Maldonado
authors.initials: JM
authors.lastname: Marchetti
mesh_terms: D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D000818:Animals; D000981:Antiprotozoal Agents / Q000627:therapeutic use*; D052117:Benzodioxoles; D014355:Chagas Disease / Q000188:drug therapy*; D003692:Delayed-Action Preparations / Q000493:pharmacokinetics / Q000627:therapeutic use*; D004146:Dioxanes; D004149:Dioxoles / Q000493:pharmacokinetics / Q000627:therapeutic use*; D004195:Disease Models, Animal; D006801:Humans; D019344:Lactic Acid / Q000493:pharmacokinetics / Q000627:therapeutic use*; D017705:Lignans / Q000493:pharmacokinetics / Q000627:therapeutic use*; D051379:Mice; D008863:Microspheres; D018512:Parasitemia / Q000188:drug therapy; D011100:Polyglycolic Acid / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D016896:Treatment Outcome; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D000981:Antiprotozoal Agents; D052117:Benzodioxoles; D003692:Delayed-Action Preparations; D004146:Dioxanes; D004149:Dioxoles; D017705:Lignans; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; C475934:hinokinin; D019344:Lactic Acid; C091880:dilactide; D015107:4-Butyrolactone