Department of Pharmaceutics, Faculty of Pharmacy, Federal University of Minas Gerais, Belo Horizonte, Minas Gerais, 31270-010, Brazil.
Department of Physiology & Biophysics, Institute of Biological Sciences, Federal University of Minas Gerais, Belo Horizonte, Minas Gerais, 31270-010, Brazil.
Nanomedicine (Lond). 2022 Aug;17(18):1237-1251. doi: 10.2217/nnm-2021-0489. Epub 2022 Oct 3.
Amphotericin B (AmB) is an antileishmanial drug with high toxicity; however, this drawback might overcome by decreasing the AmB self-aggregation state. This work aimed at evaluating the influence of cholesterol on the aggregation state of AmB loaded in a nanoemulsion (NE-AmB) for the treatment of cutaneous leishmaniasis. NE-AmB (1, 4 and 8 mg/kg/day) was administered intravenously to animals infected by every 2 days for a total of five injections. Ultraviolet-visible spectroscopy and circular dichroism studies demonstrated that cholesterol reduced AmB aggregation state in NE. NE-AmB was stable after 180 days, and its hemolytic toxicity was lower than that observed for the conventional AmB. NE-AmB administered intravenously into animals infected by at 8 mg/kg was capable of stabilizing the lesion size and reducing the parasitic load. These findings support the NE potential as a stable nanocarrier for AmB in the treatment of cutaneous leishmaniasis.
两性霉素 B（AmB）是一种具有高毒性的抗利什曼原虫药物；然而，通过降低 AmB 的自聚集状态可以克服这一缺点。本工作旨在评估胆固醇对载于纳米乳剂（NE-AmB）中用于治疗皮肤利什曼病的 AmB 聚集状态的影响。NE-AmB（1、4 和 8mg/kg/天）以每 2 天静脉注射一次的方式给予感染的动物，总共注射五次。紫外-可见光谱和圆二色性研究表明，胆固醇降低了 NE 中 AmB 的聚集状态。NE-AmB 在 180 天后保持稳定，其溶血毒性低于常规 AmB。以 8mg/kg 静脉注射给予感染 的动物的 NE-AmB 能够稳定病变大小并降低寄生虫载量。这些发现支持 NE 作为一种稳定的纳米载体用于治疗皮肤利什曼病的 AmB 的潜力。
