Borges Joyce Cordeiro, Barros Anne Beatriz Cunha, Cardoso Leonardo Lima, Keesen Tatjana de Lima Souza, Campos Luís André de Almeida, Cavalcanti Isabella Macário Ferro, Kretzschmar Elisângela Afonso de Moura
Laboratory of Industrial Nanoscience and Nanobiotechnology (LANNI), Center for Biotechnology, Federal University of Paraiba, Castelo Branco, João Pessoa, Paraiba, Brazil.
Laboratory of Immunology of Infectious Diseases (LABIDIC), Center for Biotechnology, Federal University of Paraiba, Castelo Branco, João Pessoa, Paraiba, Brazil.
Chem Biodivers. 2025 Sep;22(9):e202403341. doi: 10.1002/cbdv.202403341. Epub 2025 May 9.
Visceral leishmaniasis (VL) is a neglected parasitic disease, and the first-line treatments for VL include drugs that exhibit serious toxicological issues. In this sense, new molecules are sought for VL treatment, such as Carvacrol (Car), a phenolic monoterpene that has shown strong activity against Leishmania spp. However, its low solubility prevents its free administration, requiring a new therapeutic strategy such as encapsulation in chitosan biopolymeric nanoparticles. This study aimed to develop chitosan biopolymeric nanoparticles (NPChi) encapsulating Car (NPCar) and evaluate their in vitro anti-leishmanial activity. The NPChi had particle sizes of 89.43 ± 0.774 nm, a polydispersity index (PDI) of 0.168 ± 0.01 and zeta potential of 12.8 ± 2.17 mV. The NPCar showed particle size of 144.9 ± 1.7 nm, PDI of 0.224 and zeta potential of 15.7 ± 1.01 mV. NPCar reduced the cytotoxicity of Car on human erythrocytes. Moreover, NPCar showed inhibition of Leishmania infantum with an inhibitory concentration (IC) of 2.659 ± 0.26 µg/mL. Thus, NPCar exhibited enhanced anti-leishmanial activity compared to free Car while reducing cytotoxicity on human erythrocytes, making them promising candidates for further studies on VL treatment.
内脏利什曼病（VL）是一种被忽视的寄生虫病，VL的一线治疗药物存在严重的毒理学问题。从这个意义上说，人们正在寻找用于治疗VL的新分子，比如香芹酚（Car），一种酚类单萜，已显示出对利什曼原虫具有强大活性。然而，其低溶解度阻碍了它的直接给药，这就需要一种新的治疗策略，比如将其封装在壳聚糖生物聚合物纳米颗粒中。本研究旨在开发封装有Car的壳聚糖生物聚合物纳米颗粒（NPChi）并评估其体外抗利什曼活性。NPChi的粒径为89.43±0.774纳米，多分散指数（PDI）为0.168±0.01，zeta电位为12.8±2.17毫伏。NPCar的粒径为144.9±1.7纳米，PDI为0.224，zeta电位为15.7±1.01毫伏。NPCar降低了Car对人红细胞的细胞毒性。此外，NPCar对婴儿利什曼原虫有抑制作用，抑制浓度（IC）为2.659±0.26微克/毫升。因此，与游离Car相比，NPCar表现出增强的抗利什曼活性，同时降低了对人红细胞的细胞毒性，使其成为VL治疗进一步研究的有希望的候选药物。
