(-)-Hinokinin-loaded poly(D,-lactide-co-glycolide) microparticles for Chagas disease.
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.
Saraiva
Juliana
J
Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, Avenida do Café s/n, 14040-903 Ribeirão Preto, SP, Brazil.
Lira
Ana Amélia Moreira
AA
Esperandim
Viviane Rodrigues
VR
da Silva Ferreira
Daniele
D
Ferraudo
Antônio Sérgio
AS
Bastos
Jairo Kenupp
JK
E Silva
Márcio Luís Andrade
ML
de Gaitani
Cristiane Masetto
CM
de Albuquerque
Sérgio
S
Marchetti
Juliana Maldonado
JM
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
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