(−)−Hinokinin-loaded poly(d,l-lactide-co-glycolide) microparticles for Chagas disease

• Published in: Parasitology research (1987) Vol. 106; no. 3; pp. 703 - 708
• Main Authors: Saraiva, Juliana, Lira, Ana Amélia Moreira, Esperandim, Viviane Rodrigues, da Silva Ferreira, Daniele, Ferraudo, Antônio Sérgio, Bastos, Jairo Kenupp, e Silva, Márcio Luís Andrade, de Gaitani, Cristiane Masetto, de Albuquerque, Sérgio, Marchetti, Juliana Maldonado
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Berlin/Heidelberg : Springer-Verlag 01.02.2010; Springer-Verlag; Springer
• Subjects: 4-Butyrolactone - analogs & derivatives; 4-Butyrolactone - pharmacokinetics; 4-Butyrolactone - therapeutic use; Animals; Antiprotozoal Agents - therapeutic use; Benzodioxoles; Biological and medical sciences; Biomedical and Life Sciences; Biomedicine; Chagas disease; Chagas Disease - drug therapy; Delayed-Action Preparations - pharmacokinetics; Delayed-Action Preparations - therapeutic use; Dioxanes; Dioxoles - pharmacokinetics; Dioxoles - therapeutic use; Disease Models, Animal; drugs; encapsulation; evaporation; Fundamental and applied biological sciences. Psychology; General aspects; General aspects and techniques. Study of several systematic groups. Models; Humans; Immunology; Invertebrates; Lactic Acid - pharmacokinetics; Lactic Acid - therapeutic use; light scattering; Lignans - pharmacokinetics; Lignans - therapeutic use; Medical Microbiology; Mice; Microbiology; Microspheres; Original Paper; parasitemia; Parasitemia - drug therapy; particle size; Polyglycolic Acid - pharmacokinetics; Polyglycolic Acid - therapeutic use; scanning electron microscopy; Treatment Outcome; Trypanosoma cruzi; Trypanosoma cruzi - drug effects; Sustained Release; Drug Release Study; Lignan; Encapsulation Efficiency; PLGA Microparticle; Infection; Protozoal disease; Load; Parasite; Chagas disease; Parasitosis; Trypanosomiasis
• ISSN: 0932-0113; 1432-1955
• DOI: 10.1007/s00436-010-1725-1

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 µm 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.