Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt.
Department of Parasitology, Faculty of Medicine, Tanta University, Tanta, Egypt.
Int J Pharm. 2023 May 10;638:122912. doi: 10.1016/j.ijpharm.2023.122912. Epub 2023 Apr 2.
The goal was to scrutinize niosomes as potential carriers for enhanced efficacy of norfloxacin against Toxoplasma gondii RH strain. This was assessed in vitro and in vivo. Standard niosomes of Span 60 and cholesterol were prepared. Gelucire 48/16 or Tween 80 was incorporated as hydrophilic fluidizer. The prepared vesicles were characterized for shape, size, viscosity and norfloxacin release. The in vitro anti-Toxoplasma was assessed by monitoring tachyzoites viability after incubation with niosomes. In vivo efficacy of niosomes encapsulated norfloxacin was evaluated on infected mice. Transmission electron micrographs showed nano-sized spherical vesicles. Norfloxacin release varied with niosomal composition to show faster liberation in presence of fluidizing agent. The half maximum effective concentration of norfloxacin against tachyzoites (EC50) was significantly reduced after niosomal encapsulation compared with simple drug solution with no significant difference between vesicular formulations. Tachyzoite count in the peritoneal fluid of infected mice was reduced by 45.2, 90.8, 88.3 and 84% after treatment with simple drug dispersion, standard niosomes, Gelucire containing and Tween containing vesicles, respectively compared to infected untreated mice. These results correlate with the in vitro data and reflects the efficacy of niosomes. The study introduced surfactant vesicles as a tool for enhanced efficacy of norfloxacin against toxoplasma.
目的是研究诺氟沙星奈脂质体作为增强抗弓形虫 RH 株疗效的潜在载体。这是在体外和体内进行评估的。制备了 Span 60 和胆固醇标准奈脂质体。加入亲水性增塑剂 Gelucire 48/16 或吐温 80。对制备的囊泡进行形状、大小、粘度和诺氟沙星释放的特征描述。通过孵育后监测速殖子活力来评估体外抗弓形虫活性。用感染的小鼠评估包封诺氟沙星的奈脂质体的体内疗效。透射电镜照片显示纳米尺寸的球形囊泡。诺氟沙星的释放随奈脂质体的组成而变化，在存在增塑剂的情况下释放更快。与简单药物溶液相比，诺氟沙星对速殖子的半最大有效浓度（EC50）在奈脂质体包封后显著降低，而囊泡制剂之间没有显著差异。与感染未治疗的小鼠相比，用简单药物分散剂、标准奈脂质体、含 Gelucire 的囊泡和含吐温的囊泡处理感染的小鼠后，腹腔液中的速殖子计数分别减少了 45.2%、90.8%、88.3%和 84%。这些结果与体外数据相关，反映了奈脂质体的疗效。该研究介绍了表面活性剂囊泡作为增强诺氟沙星抗弓形虫疗效的工具。
