Development of Novel Oral Extended-Release Anthelmintic Formulations for Grazing Cattle
摘要
Ireland is a globally recognised trading nation, providing high-quality meat, milk, and dairy products. To remain viable and grow over time, the Irish agricultural sector must prioritise animal health to maximise productivity, as parasite infections represent a major production-limiting issue.
ObjectiveThis study aimed to formulate plasticised solid dispersion tablets containing oxfendazole (OXF), a broad-spectrum benzimidazole anthelmintic, with improved dissolution behaviour and an extended-release profile. The work addresses the challenge posed by the poor aqueous solubility and limited dissolution of OXF, factors that restrict its therapeutic performance, and introduces a semi-continuous manufacturing strategy to overcome these limitations.
MethodsAn innovative pharmaceutical approach employing a semi-continuous manufacturing process that integrates hot-melt extrusion (HME) with micro-injection moulding (µIM) was investigated. Two solid dispersion formulations were developed and evaluated: SDF 1, consisting of PEO 95% and OXF 5% (w/w), and SDF 2, consisting of PEO 52.3%, OXF 2.7%, and PCL 45% (w/w/w).
ResultsIn vitro drug release studies using high-performance liquid chromatography (HPLC) showed that SDF 1 achieved an ~ 8-fold enhancement in drug dissolution compared to a commercial OXF tablet. SDF 2 demonstrated a ~ 4-fold increase in drug release over a three-day period, attributable to its extended-release characteristics. Biocompatibility was assessed through cell viability assays, confirming that the plasticised tablets produced by melt-processing techniques are non-toxic.
ConclusionHME coupled with µIM are novel pharmaceutical manufacturing techniques with potential to scale up to mass production. These advanced OXF formulations present a promising therapeutic strategy for the control of helminthiasis in grass-fed cattle, supporting enhanced animal health and agricultural sustainability.