College of Pharmacy and Health Sciences, St. John's University, Queens, NY, United States.
College of Pharmacy and Health Sciences, St. John's University, Queens, NY, United States.
Int J Pharm. 2022 Oct 15;626:122163. doi: 10.1016/j.ijpharm.2022.122163. Epub 2022 Sep 5.
Fascioliasis, a common parasitic infection observed in the pediatric patient population, is a leading cause of concern in countries with poor/unhealthy water resources. To treat this condition first line agent such as triclabendazole (TBZ) has been the choice therapy. However, there is a major hurdle in exploiting TBZ. Characterized with poor aqueous solubility (0.1 mg/L), its solubility has been the rate limiting factor, rendering requirement of large doses of TBZ. To address the same, the focus of the current study was to develop a self-nano emulsifying drug delivery system (TBZ-SNEDDS) for TBZ and developing dose customizable pediatric dispersible color-coded tablets. TBZ-SNEDDS were successfully formulated by using Kolliphor®EL, as a surfactant, a lipid phase of medium chain triglyceride and α-tocopherol in the ratio of (1:1), with dimethylacetamide (DMA) as a solvent. It was observed during in vitro release studies that there was a significant effect of fed conditions on the rate of TBZ release from the formulation. greater than 85 % TBZ was observed to release in fed conditions in comparison to fasted conditions. As currently TBZ is prescribed on a weight-based dosage regimen, it is imperative to develop a dose-customizable fast dissolving pediatric formulation. Hence, TBZ-SNEDDS could prove to be pivotal in helping countless children around the world in desperate conditions to get cheap yet effective therapy.
肝片形吸虫病是一种常见的寄生虫感染,在水资源较差/不健康的国家是一个主要的关注点。治疗这种疾病的一线药物如三氯苯达唑(TBZ)一直是首选治疗方法。然而,在开发 TBZ 时存在一个主要障碍。其水溶性差(0.1mg/L),溶解度是限速因素,需要使用大剂量的 TBZ。为了解决这个问题,目前的研究重点是开发 TBZ 的自微乳给药系统(TBZ-SNEDDS),并开发可定制剂量的儿科分散片。通过使用 Kolliphor®EL 作为表面活性剂、中链甘油三酯和 α-生育酚的脂质相(1:1),并使用二甲基乙酰胺(DMA)作为溶剂,成功地制备了 TBZ-SNEDDS。在体外释放研究中观察到,给食条件对制剂中 TBZ 释放速率有显著影响。与空腹条件相比,在给食条件下,超过 85%的 TBZ 被释放。由于目前 TBZ 是根据体重剂量方案开处方的,因此开发一种可定制剂量的快速溶解儿科制剂势在必行。因此,TBZ-SNEDDS 可以帮助世界上无数处于困境中的儿童获得廉价而有效的治疗。