Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, Avenida do Café s/n, 14040-903 Ribeirão Preto, SP, Brazil.
Parasitol Res. 2010 Feb;106(3):703-8. doi: 10.1007/s00436-010-1725-1. Epub 2010 Jan 28.
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.
(-)-扁柏酚显示出对体外和体内 Trypanosoma cruzi 的高活性。为了保护 (-)-扁柏酚免受生物相互作用的影响并促进其持续释放以治疗恰加斯病，制备并表征了负载 (-)-扁柏酚的聚(D,L-丙交酯-共-乙交酯)微球。通过乳液/溶剂蒸发的经典方法制备负载 (-)-扁柏酚的微球。使用扫描电子显微镜和光散射分析仪分别研究形态和粒径。测定包封效率，进行动力学评估药物释放研究，并进行体内抗锥虫作用评价。获得的负载 (-)-扁柏酚的微球平均直径为 0.862 微米，表面光滑，呈球形。包封效率为 72.46 +/- 2.92%，开发的系统以 Higuchi 动力学维持药物释放。该制备方法是合适的，因为形态特征、包封效率和体外释放曲线令人满意。体内试验表明，给予负载 (-)-扁柏酚的微球后，小鼠寄生虫血症显著减少。因此，开发的微球似乎是一种有前途的持续释放 (-)-扁柏酚治疗恰加斯病的系统。
