Development of a safe pediatric liquisolid self-nanoemulsifying system of triclabendazole for the treatment of fascioliasis

Int J Pharm. 2022 Oct 15:626:122163. doi: 10.1016/j.ijpharm.2022.122163. Epub 2022 Sep 5.

Abstract

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.

Keywords: Dose Customization; Pediatric formulations; Self-Nanoemulsifying Preconcentrate; Triclabendazole.

MeSH terms

  • Biological Availability
  • Child
  • Drug Delivery Systems
  • Emulsions
  • Fascioliasis*
  • Humans
  • Lipids
  • Nanoparticles*
  • Particle Size
  • Solubility
  • Solvents
  • Surface-Active Agents
  • Tablets
  • Triclabendazole
  • Triglycerides
  • alpha-Tocopherol

Substances

  • alpha-Tocopherol
  • Emulsions
  • Lipids
  • Solvents
  • Surface-Active Agents
  • Tablets
  • Triclabendazole
  • Triglycerides