Institute of Biophysics Carlos Chagas Filho, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
Institute of Macromolecules Eloisa Mano, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
Am J Ther. 2019 Jan/Feb;26(1):e12-e17. doi: 10.1097/MJT.0000000000000539.
Leishmaniasis is a neglected disease endemic in tropical and subtropical areas, with an incidence about 1.6 million cases/year. The first-line treatment of this disease is pentavalent antimony, and the second-line are pentamidine and amphotericin B. All the treatments available cause severe side effects and often have difficulty in accessing parasites within infected cells.
This study aimed to determine if the use of nanoparticles loaded with meglumine antimoniate could reach and targeting infected organs with leishmaniasis, reducing the dosage used and promoting less adverse effects.
This study was performed comparing the meglumine nanoparticle in two experimental groups. The first one healthy mice and the second one inducted mice (leishmaniasis).
The nanoparticles loaded with meglumine antimoniate (nanoantimony) were prepared by double-emulsion solvent evaporation method and showed a size of about 150-200 nm. BALB/c mice infected or not with Leishmania amazonensis (cutaneous leishmaniasis model) or Leishmania infantum (visceral leishmaniasis model) was used to access the biodistribution of nanoantimony and meglumine antimoniate labeled with technetium-99m.
The biodistribution profiles showed a preferential targeting of the nanoparticles to the liver, spleen, and lungs. Because these are the main organs infected, the nanoparticle may be used for this purpose. The results for cutaneous leishmaniasis showed a low uptake by the lesion (infected region).
The results demonstrated the potential use of these nanoparticles to improve the efficacy of meglumine antimoniate in the treatment of visceral leishmaniasis, indicating their potential as an alternative therapeutic strategy for leishmaniasis infections.
利什曼病是一种在热带和亚热带地区流行的被忽视疾病，每年发病率约为 160 万例。该疾病的一线治疗药物是五价锑，二线治疗药物是喷他脒和两性霉素 B。所有现有的治疗方法都会引起严重的副作用，而且往往难以进入感染细胞内的寄生虫。
本研究旨在确定是否可以使用负载葡甲胺锑的纳米颗粒来达到并靶向利什曼病感染的器官，减少使用剂量并减少不良反应。
本研究比较了两种实验性葡甲胺纳米颗粒组。第一组是健康小鼠，第二组是诱导的（利什曼病）小鼠。
通过双乳液溶剂蒸发法制备负载葡甲胺锑的纳米颗粒（纳米锑），粒径约为 150-200nm。使用 BALB/c 小鼠感染或未感染利什曼原虫（皮肤利什曼病模型）或利什曼原虫（内脏利什曼病模型），以评估纳米锑和标记锝-99m 的葡甲胺的生物分布。
生物分布图谱显示纳米颗粒优先靶向肝脏、脾脏和肺部。因为这些是主要感染的器官，纳米颗粒可能被用于这个目的。对于皮肤利什曼病，病变（感染区域）的摄取量较低。
结果表明，这些纳米颗粒有可能改善葡甲胺锑治疗内脏利什曼病的疗效，表明它们有潜力成为利什曼病感染的替代治疗策略。
