State University of Goias, Anapolis, Goias, Brazil.
Tropical Pathology and Public Health Institute, Federal University of Goias, Goiania, Goias, Brazil.
Drug Deliv Transl Res. 2018 Oct;8(5):1265-1273. doi: 10.1007/s13346-018-0576-7.
Neurocysticercosis is the most common parasitic infection of the nervous system and currently represents a serious public health issue in many regions of Latin America, Asia, and Africa. To date, praziquantel is one of the chosen drugs for the treatment of neurocysticercosis. Its mechanism of action is based on the inhibition of different biochemical pathways within the parasite which contribute to its death. Thus, the aim of this work was to analyze, for the first time, whether the nanoformulations of praziquantel would modify the energetic pathway of Taenia crassiceps cysticerci, after an intracranial inoculation in BALB/c mice. Praziquantel nanosuspensions were formulated with polyvinyl alcohol, poloxamer 188, and poloxamer 407, as stabilizers. These formulations exhibited particle size in a range of 74-285 nm and zeta potential values in a range of - 8.1/- 13.2 depending on the type of stabilizer. Physical stability study at both 4 ± 2 and 25 ± 2 °C indicated that praziquantel (PZQ) nanoparticles were stable in terms of solubility and particle size after 120-day storage. In vivo studies demonstrated that those nanosystems were able to produce significant modifications on the concentrations of oxaloacetate, citrate, pyruvate, alpha-ketoglutarate, malate, succinate, lactate, beta-hydroxybutyrate, fumarate, and propionate involved in the metabolism of Taenia crassiceps cysticerci. Therefore, these nanoformulations may be considered as a promising tool to deliver praziquantel to the brain for the effective management of neurocysticercosis.
脑囊尾蚴病是最常见的神经系统寄生性感染，目前在拉丁美洲、亚洲和非洲的许多地区都是严重的公共卫生问题。到目前为止，吡喹酮是治疗脑囊尾蚴病的首选药物之一。其作用机制基于抑制寄生虫内的不同生化途径，这些途径有助于寄生虫的死亡。因此，本工作的目的是首次分析吡喹酮的纳米制剂是否会在 BALB/c 小鼠颅内接种后改变猪带绦虫囊尾蚴的能量途径。吡喹酮纳米混悬剂用聚乙烯醇、泊洛沙姆 188 和泊洛沙姆 407 作为稳定剂进行了配方设计。这些制剂的粒径在 74-285nm 范围内，zeta 电位值在-8.1/-13.2 范围内，具体取决于稳定剂的类型。在 4±2℃和 25±2℃下的物理稳定性研究表明，吡喹酮（PZQ）纳米颗粒在 120 天储存后在溶解度和粒径方面是稳定的。体内研究表明，这些纳米系统能够对参与猪带绦虫囊尾蚴代谢的草酰乙酸、柠檬酸、丙酮酸、α-酮戊二酸、苹果酸、琥珀酸、乳酸、β-羟丁酸、富马酸和丙酸盐的浓度产生显著的改变。因此，这些纳米制剂可以被认为是将吡喹酮递送到大脑以有效治疗脑囊尾蚴病的有前途的工具。
